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Study Guide: Chemistry of Free Bases and Related Applications

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Chemistry of Free Bases and Related Applications Study Guide

Chemical Fundamentals of Free Bases

A free base is defined as the protonated or salt form of a Lewis base molecule.

Answer: False

Explanation: A free base is defined as the neutral form of a molecule, specifically an amine or other Lewis base, not its protonated or salt form.

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In chemistry, a Lewis base is characterized by its ability to accept an electron pair.

Answer: False

Explanation: A Lewis base is characterized by its ability to donate an electron pair, not accept one.

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Hydroxylamine hydrochloride represents the neutral, free base form of hydroxylamine.

Answer: False

Explanation: Hydroxylamine hydrochloride represents the salt form (NH3OH+ Cl−), while the neutral, free base form of hydroxylamine is NH2OH.

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The image caption "Lewis bases and acids" refers to a theory where bases accept electron pairs and acids donate them.

Answer: False

Explanation: The Lewis theory defines bases as electron-pair donors and acids as electron-pair acceptors.

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The primary chemical characteristic defining a free base is its ionic nature.

Answer: False

Explanation: The primary characteristic defining a free base is its neutral, non-ionic nature, as opposed to its protonated or salt form.

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According to the chemical definition provided, what is a "free base"?

Answer: The neutral form of an amine or other Lewis base.

Explanation: A free base is chemically defined as the neutral form of an amine or other Lewis base, contrasting with its protonated or salt state.

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The caption "Lewis bases and acids" relates to a chemical theory where:

Answer: Bases donate electron pairs and acids accept electron pairs.

Explanation: The Lewis theory defines Lewis bases as substances capable of donating electron pairs and Lewis acids as substances capable of accepting electron pairs.

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How does the colloquial understanding of "free-basing" differ from the pharmaceutical definition?

Answer: Pharmaceutical: neutral form; Colloquial: smoking process.

Explanation: The pharmaceutical definition refers to the neutral chemical form, while the colloquial understanding of "free-basing" pertains to the recreational process of smoking a drug's free base form.

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Properties and Synthesis of Free Bases

The pharmaceutical industry uses the term "free base" to refer exclusively to the drug's salt form for enhanced stability.

Answer: False

Explanation: In the pharmaceutical industry, "free base" denotes the neutral chemical form of a substance, distinct from its salt forms, which may be preferred for stability or solubility.

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Amine salts generally have lower water solubility compared to their corresponding free base forms.

Answer: False

Explanation: Amine salts generally exhibit greater water solubility compared to their corresponding free base forms.

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The source indicates that certain alkaloids exhibit greater stability when in their ionic salt form compared to their neutral free base form.

Answer: True

Explanation: Some alkaloids may exhibit greater stability when in their ionic salt form compared to their neutral free base form, although salts often have higher water solubility.

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Hydrochloric acid is the only acid used to form salts with amines.

Answer: False

Explanation: Various acids, including sulfuric, phosphoric, nitric, acetic, oxalic, citric, and tartaric acids, can be used to form salts with amines, not solely hydrochloric acid.

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How does the pharmaceutical industry typically utilize the term "free base"?

Answer: To denote the neutral chemical form of a substance, distinct from its salts.

Explanation: In the pharmaceutical context, "free base" refers to the neutral chemical form of a substance, differentiating it from its salt forms which may be used for formulation purposes.

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What is a primary difference in chemical properties between amine salts and their free base forms, according to the source?

Answer: Salts typically exhibit greater water solubility than free bases.

Explanation: A primary difference is that amine salts, such as hydrochlorides, typically exhibit greater water solubility compared to their corresponding free base forms.

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What is a hydrochloride, in the context of amine salts?

Answer: A salt formed when an amine reacts with hydrochloric acid.

Explanation: A hydrochloride is specifically a salt formed when an amine undergoes an acid-base reaction with hydrochloric acid.

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Which of the following is NOT listed as a common counterion used when forming amine salts?

Answer: Carbonate

Explanation: The provided list of common counterions for amine salts includes chloride, bromide, sulfate, phosphate, nitrate, acetate, oxalate, citrate, and tartrate. Carbonate is not listed.

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Cocaine: Chemistry, Preparation, and Forms

Cocaine hydrochloride is preferred for smoking due to its low melting point and volatility.

Answer: False

Explanation: Cocaine hydrochloride decomposes when subjected to the high temperatures of smoking and is therefore unsuitable for this method of administration; free base cocaine is preferred due to its volatility.

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Free base cocaine can be vaporized and inhaled because it becomes volatile above 90°C.

Answer: True

Explanation: Free base cocaine has a relatively low melting point and becomes volatile above 90°C, allowing it to be vaporized and inhaled when smoked.

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The freebasing process helps remove water-soluble adulterants like sugars from street cocaine.

Answer: True

Explanation: The process of freebasing serves as a purification method, effectively removing water-soluble adulterants such as sugars (e.g., lactose) commonly found in street cocaine.

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Free base cocaine is significantly more soluble in water than cocaine hydrochloride.

Answer: False

Explanation: Cocaine hydrochloride is highly soluble in water, whereas free base cocaine exhibits very low solubility in water.

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The preparation of free base cocaine involves dissolving the hydrochloride salt in an alkaline solution and then extracting it with a polar solvent.

Answer: False

Explanation: The preparation involves dissolving the hydrochloride salt in an alkaline solution and then extracting the resulting free base with a non-polar solvent, not a polar one.

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Trituration is a method where cocaine hydrochloride is heated in water with a base to convert it into free base cocaine.

Answer: True

Explanation: Trituration is a technique involving the dissolution of cocaine hydrochloride in water with heat and the addition of a base, facilitating its conversion to the free base form.

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Crack cocaine is the common name for the purified, crystalline form of free base cocaine produced through cooking or trituration.

Answer: True

Explanation: Crack cocaine is the widely recognized name for the solid, rock-like substance resulting from the purification and preparation of free base cocaine via methods such as cooking or trituration.

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In the preparation of free base cocaine, an alkaline solution converts the cocaine hydrochloride into its free base form, which is then dissolved by a non-polar solvent.

Answer: True

Explanation: The process involves using an alkaline solution to convert cocaine hydrochloride to its free base, which is subsequently dissolved and separated using a non-polar solvent.

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The process of "cooking" cocaine hydrochloride involves converting it into crack cocaine, a smokable form.

Answer: True

Explanation: The process commonly referred to as "cooking" cocaine hydrochloride transforms it into crack cocaine, a smokable form of free base cocaine.

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Why is cocaine hydrochloride unsuitable for smoking?

Answer: It decomposes when subjected to the high temperatures of smoking.

Explanation: Cocaine hydrochloride decomposes upon exposure to the high temperatures involved in smoking, rendering it unsuitable for this administration route.

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What property of free base cocaine makes it suitable for smoking?

Answer: It becomes volatile and can be vaporized at temperatures above 90°C.

Explanation: Free base cocaine becomes volatile and can be vaporized at temperatures above 90°C, a property that facilitates its administration via smoking.

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Which of the following substances is often removed from street cocaine during the freebasing process?

Answer: Water-soluble sugars such as lactose

Explanation: The freebasing process helps purify cocaine by removing water-soluble adulterants, including sugars like lactose, sucrose, and glucose.

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How does the water solubility of cocaine freebase compare to cocaine hydrochloride?

Answer: Free base is significantly less soluble than the hydrochloride.

Explanation: Cocaine hydrochloride is highly soluble in water (approx. 1 part in 0.5), whereas cocaine freebase exhibits very low water solubility (approx. 1 part in 600).

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In the chemical extraction method for free base cocaine, what is the role of the non-polar solvent?

Answer: To dissolve and separate the free base cocaine from the aqueous layer.

Explanation: The non-polar solvent is used to dissolve the free base cocaine after it has been formed by the alkaline solution, allowing it to be separated from the aqueous layer.

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What is the common name for the solid, rock-like substance produced when preparing free base cocaine through "cooking" or trituration?

Answer: Crack cocaine

Explanation: The solid, rock-like substance resulting from the preparation of free base cocaine through methods like cooking or trituration is commonly known as crack cocaine.

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Which chemical process is described for preparing free base cocaine from its hydrochloride salt?

Answer: Reaction with a base and extraction using a non-polar solvent.

Explanation: The preparation involves reacting cocaine hydrochloride with a base to form the free base, which is then extracted using a non-polar solvent.

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What is trituration in the context of preparing free base cocaine?

Answer: A process of dissolving cocaine hydrochloride in water with heat and base.

Explanation: Trituration, in this context, refers to a method where cocaine hydrochloride is heated in water with a base to convert it into free base cocaine.

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Which of the following best describes the difference between free base cocaine and cocaine hydrochloride regarding smoking?

Answer: Free base is volatile; hydrochloride decomposes.

Explanation: Free base cocaine is volatile and can be vaporized for smoking, whereas cocaine hydrochloride decomposes at smoking temperatures and is unsuitable for this method.

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The process of converting cocaine hydrochloride using an alkaline solution and a non-polar solvent yields a product that is:

Answer: The neutral free base form of cocaine.

Explanation: This chemical process converts cocaine hydrochloride into its neutral free base form.

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Physiological and Pharmacological Interactions

The body's blood chemistry, specifically its buffering system, causes inhaled free-base amines to remain in their neutral form.

Answer: False

Explanation: The blood's natural buffering system, operating at physiological pH, causes inhaled free-base amines to revert to their protonated, or acid, form.

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At physiological pH (7.4), approximately 94.19% of cocaine exists in its protonated (acid) form.

Answer: True

Explanation: Based on a pKa of 8.61 for cocaine and a physiological blood pH of 7.4, calculations indicate that approximately 94.19% of cocaine exists in its protonated (acid) form.

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Le Chatelier's principle suggests that the removal of free-base cocaine from the brain causes the equilibrium to shift towards forming *more* free base.

Answer: True

Explanation: Le Chatelier's principle explains that the continuous utilization or removal of free-base cocaine from the brain shifts the equilibrium, prompting the protonated (acid) form in the blood to convert back into the free base, thus maintaining its presence.

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How does the body's blood chemistry affect the form of inhaled free-base amines?

Answer: It converts them back into their protonated, or acid, form.

Explanation: Upon entering the bloodstream, inhaled free-base amines are rapidly converted back into their protonated, or acid, form due to the body's physiological buffering system.

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Based on the provided pKa for cocaine (8.61) and physiological pH (7.4), what is the approximate state of cocaine in the blood?

Answer: Almost entirely in its acid (protonated) form.

Explanation: Given that the physiological blood pH (7.4) is below cocaine's pKa (8.61), the substance predominantly exists in its protonated, or acid, form in the blood.

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Le Chatelier's principle explains the sustained presence of free-base cocaine in the brain by describing how:

Answer: Utilization or removal of the free base form shifts the equilibrium, causing more acid form to convert.

Explanation: Le Chatelier's principle explains that the continuous utilization or removal of free-base cocaine from the brain shifts the equilibrium, prompting the protonated (acid) form in the blood to convert back into the free base, thus maintaining its presence.

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What is the primary reason the acid (protonated) form of cocaine predominates in the blood?

Answer: The blood pH is lower than cocaine's pKa.

Explanation: The physiological blood pH (7.4) is lower than cocaine's pKa (8.61), which dictates that the substance will predominantly exist in its protonated, or acid, form.

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What chemical principle explains why the brain can maintain a supply of free-base cocaine even after it enters the bloodstream in that form?

Answer: Le Chatelier's principle

Explanation: Le Chatelier's principle explains the sustained presence of free-base cocaine in the brain by describing how its utilization shifts equilibrium, causing more of the protonated form to convert to the free base.

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Historical and Cultural Contexts of Use

Colloquially, "free-basing" refers to the process of converting a drug into its neutral form for recreational smoking.

Answer: True

Explanation: The colloquial term "free-basing" specifically denotes the process of converting a drug's salt form into its neutral free base form, typically for the purpose of recreational smoking.

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The practice of smoking cocaine base first appeared in the United States around 1975.

Answer: False

Explanation: The practice of smoking cocaine base first emerged in the United States in 1974.

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Upon its emergence in the US, the smoking of cocaine base was initially most prevalent in New York.

Answer: False

Explanation: Initially, the smoking of cocaine base was most prevalent in California upon its appearance in the United States.

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In 1975, the first recorded hospital admission related to free-basing coincided with the commercial availability of related accessories.

Answer: True

Explanation: The year 1975 marked the first recorded hospital admission associated with free-basing, occurring concurrently with the commercial availability of extraction kits and smoking accessories.

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Between 1979 and 1982, the percentage of cocaine-related hospital admissions involving free base use decreased from 7% to 1%.

Answer: False

Explanation: Between 1979 and 1982, the percentage of cocaine-related hospital admissions involving free base use increased, rising from 1% to 7%.

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Traditional consumption of coca leaves in South America involves chewing them with an acidic substance.

Answer: False

Explanation: Traditional consumption of coca leaves in South America involves chewing them with an alkaline substance, such as llipta.

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Coca paste, known as basuco, is a substance used in South America that is frequently confused with cocaine freebase.

Answer: True

Explanation: Coca paste, also known as basuco, is an inexpensive substance used in South America and is often confused with cocaine freebase in North America.

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Chewing betel nuts involves adding an alkaline substance to convert arecoline into its freebase form for better absorption.

Answer: True

Explanation: When betel nuts are chewed, an alkaline substance like limestone is typically added, which converts the active compound arecoline into its freebase form, enhancing absorption.

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When did the practice of smoking cocaine base first emerge in the United States?

Answer: 1974

Explanation: The practice of smoking cocaine base first emerged in the United States in the year 1974.

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Which U.S. state was initially the primary location for the prevalence of cocaine base smoking upon its appearance?

Answer: California

Explanation: Upon its emergence in the United States, the smoking of cocaine base was initially most prevalent in California.

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What significant event related to free-basing occurred in 1975?

Answer: The first recorded hospital admission related to free-basing occurred.

Explanation: The year 1975 saw the first recorded hospital admission related to free-basing, coinciding with the commercial availability of related accessories.

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How did hospital admissions related to free base cocaine use change between 1979 and 1982?

Answer: They increased, with the percentage rising from 1% to 7%.

Explanation: Between 1979 and 1982, hospital admissions related to free base cocaine use increased significantly, with the percentage rising from 1% to 7%.

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What alkaline substance is traditionally used when chewing coca leaves in South America?

Answer: Llipta

Explanation: Traditionally, coca leaves are chewed in South America with an alkaline substance known as 'llipta,' often derived from plant ashes or shells.

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How does the addition of limestone enhance the effect when chewing betel nuts?

Answer: It converts arecoline into its freebase form, aiding absorption.

Explanation: Adding limestone, an alkaline substance, converts the arecoline in betel nuts into its freebase form, which enhances its absorption through sublingual tissues.

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What is "coca paste" (basuco)?

Answer: An inexpensive substance used in South America, often confused with cocaine freebase.

Explanation: Coca paste, also known as basuco, is an inexpensive substance widely used in South America and is frequently mistaken for cocaine freebase.

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