Amphetamine Syntheses Overview & Reference Guide for Professionals (Psychoactive Synthesis Series Vol 1)

278 Pages·1998·78.06 MB·English

by  Otto Snow

AMPHETAMINE
SYNTHESES
OVERVIEW
&
REFERENCE GUIDE FOR
PROFESSIONALS
by OTTO SNOW
PSYCHOACTIVE
SYNTHESIS SERIES
VOLUME 1
AMPHETAMINE SYNTHESES
THOTH PRESS
P.O. Box 6081
Spring Hill, FI 3461 1
Copyright © 1998 Otto Snow
All rights reserved. No part of this book maybe reproduced, in
part or in whole without prior written permission from author.
The reference guide may not be stored, transferred by electronic
means or any other forms of data storage or transfer.
Made and printed in the United States of America
ISBN: 0-9663128-0-5
Library of Congress Catalog Card Number: 98-90044
Materials contained within this volume prepared for and
appearing in government documentation are not covered by
above-mentioned copyright. The source of brief excerpts from
previously published materials is credited and not covered under
above-mentioned copyright.
Cover design graphics by Ted Stockowski at:
www.looking-glass.com/Majestic
e-mail [email protected]
I I
AMPHETAMINE SYNTHESES
DEDICATION
I dedicate this book to my father: Harry Snow (1921 - 1994)
I am in appreciation of: L. Lewin, E. Spath, A. Heffter, G. Alles, A.
Shulgin, C. Naranjo, T. Sargent, D. Nichols, G. Greer, and all those
explorers (too numerous to name) who opened a path into the great
unknown, unraveling the mysteries of the brain-mind.
I also want to acknowledge those who unravel the mysteries of
the galaxies, stars and beyond, namely Carl Sagan, Copernicus and
Galileo.
I want to thank the following: National Institute on Drug Abuse
for their publications and help in locating specific toxicological studies;
the Drug Enforcement Administration, Office of Intelligence, for their
statistics on drug laboratory seizures; Eric Sterling of the Criminal
Justice Policy Foundation for directing me to look into the Congressional
Hearings prior to the passage of Analogue Act of 1986; Alexander
Shulgin for his insight & words of encouragement.
"(If) every public action which is not customary, either is wrong
or, if it is right, is a dangerous precedent.
It follows that nothing should ever be done for the first time."
Cornford 1 908
"Nothing will ever be attempted
if all possible objections must be first overcome."
Samuel Johnson (1709-1784)
"Question: ... the rats are saying it (MDMA) seems to be
amphetamine-like but, in fact, it really is not ... "
"Obviously no one knows what the rats are thinking ... "
Richard A. Glennon 1 988
"Recreation is therapy; at least that's what people tell me."
Otto Snow 19 92
"Fill the seats of justice with good men,
not so absolute in goodness as to forget what human frailty is."
Sir Thomas Noon Talfourd
III
AMPHETAMINE SYNTHESES
THBLE OF CONTENTS
Chapter Page
Dedication------------------------------- III
Reader's Notice-------------------------- x
I ntroduction----------------------------- ' xi
1 Psychopharmaceutical Trade-------------- 1
2 The History of Psychoactiue Chemistry----- 7
3 Designer Drugs--------------------------- 13
Controlled Substance Analogue Act--------- 21
4 The Two Prong Attack:--------------------- 22
The First Prong--------------------------- 22
Substantial Differences in Phenylethylamines
A Change in Structure; A Change in Activity-- 22
Substantial Differences in Amphetamines
A Change in Structure; A Change in Activity-- 23
The Same Molecule, Different Species,
Different Activity------------------------ 25
The Second Prong------------------------- 27
"Intended For Human Consumption" --------- 27
5 The Repression of Neurochemistry-------- 31
A Functional Knowledge of Chemicals------- 34
6 The Chemistry--------------------------- 39
Molecular Weights;
(Moles); The Keys of Chemistry------------- 41
Decade of the Brain Proclamation--------- 44
7 Psychoactiue Substances----------------- 46
Mescaline & Other Psychoactive
Phenylethylamines------------------------ 46
Amphetamines, Methylamphetamine
& Substituted Phenylisopropylamines------- 52
IV
AMPHETAMINE SYNTHESES
Chapter Page
Ephedrine Alkaloids----------------------- 58
Aminoketones; Cathinones----------------- 61
8 Reductions------------------------------ 63
Reduction of Phenyl-Z-propanone Using
Aluminum Amalgam and Amine Solution----- 63
Reduction of Phenyl-Z-propanone Using
Aluminum Turnings, Mercuric Bichloride
and Amine Solution----------------------- 64
Reduction of Phenyl-Z-propanone Using
Aluminum Amalgam with Nitroalkane------- 65
Phenylethylamines from B-Nitrostyrene,
Zinc, and Mercuric Bichloride--------------- 66
Reduction of Phenylnitroalcohols
with Use of Zinc-------------------------- 67
Preparation of Aluminum Amalgam---------- 68
Preparation of Mercury Bichloride---------- 69
Electrolytic Reduction Apparatus----------- 70
Electrolytic Reduction Apparatus Components 70
The Electrolytic Reduction----------------- 73
Drying of the Phenylalkylamine HCI--------- 77
Purification and Precipitation of the
Substituted Phenylalkylamine Salt---------- 77
Purification of the Crude Phenylalkylamine
HCI Salt From the Catholyte Liquor---------- 77
9 Phenyl-2-nitropropene Preparation
Phenylnitroalkenes From Benzaldehydes
and Nitroalkanes-------------------------- 78
Preparation of Phenylnitroalcohols--------- 82
Pseudonitrosites From
Substituted Propenylbenzenes-------------- 84
v
AMPHETAMINE SYNTHESES
Chapter Page
Phenyl-2-nitropropenes From
Pseudonitrosites------------------------- 85
1-(Phenyl)-1-acetoxy-2-nitropropane
From Propenylbenzene--------------------- 87
10 Preparation of Phenyl-2-Propanone--- ---- 88
Phenyl-2-propanone From Phenylacetic Acid- 88
P-2-P From Phenyl-2-Nitropropenes-------- 89
P-2-P From Monochloroacetone------------- 91
Preparation of Monochloroacetone---------- 92
Phenyl-l,2-Propanediol Diacetates
From Propenylbenzenes-------------------- 93
P-2-P From Phenyl-l,2-Propanediol
Diacetates------------------------------- 94
Friedel-Crafts Reaction; Ketones From Phenols 94
11 Preparation of Rlpha-Methylphenylalanines
From Phenyl-2-Propanones--------------- 96
12 Rmphetamines From
Phenylisopropyl-N-Formamides----------- 100
Phenylisopropyl-N-Formamides From:
(A) Leuckart-Wallach Reaction;
P-2-P and Ammonium Formate------------- 102
(8) P-2-P and Formamides----------------- 103
(C) Ritter Reaction; Allybenzene or
Phenyl-2-propanol and Sodium Cyanide------ 105
alpha-Methyl-Phenylpropionamide From
alpha-Methyl-Phenylpropionic Acid--------- 106
Willgerodt Reaction: B-Phenylpropionamide
from various Starting Molecules------------ 107
Hofmann Reaction: Amphetamine from
alpha-Methyl-Phenylpropionamide---------- 108
VI
AMPHETAMINE SYNTHESES
Chapter Page
13 Rmphetamines From
Phenyl-2-Bromopropane----------------- 110
Phenyl-2-Bromopropane from Allybenzenes-- 111
14 Norpseudoephedrine (Kathine) From
Phenylpropanolamine-------------------- 113
Norpseudoephedrine From N-Acetyl-Phenyl
propanolamine---------------------------- 114
N-Acetyl-Phenylpropanolamine
From Phenylpropanolamine----------------- 115
Phenyl-1 -chloro-1 -amino-2-propane
from Phenylpropanolamine----------------- 116
15 Preparation of Rminoketone
Preparation of alpha-Bromopropiophenone--- 117
Preparation of alpha-Methylaminopropiophenone
from alpha-Bromopropiophenone------------ 118
16 Benzaldehydes-------------------------- 119
Benzaldehydes From Phenols; Duff Reaction-- 123
Benzaldehydes from Phenols; Elbs Persulfate
Oxidation-------------------------------- 125
Phenols From Benzaldehydes; Dakin Reaction- 126
Mono-Alkylation of Hydroxybenzaldehydes--- 127
Benzaldehydes From Propenylbenzenes------ 128
17 Substituted Phenylpropenes-------------- 130
Ally and propenyl benzenes from
Natural Sources-------------------------- 130
Propenylbenzenes From Phenyl-1 -Propanols- 136
Allybenzene From 3-Phenyl-1 -propanol By
Thermal Dehydration---------------------- 137
Propenyl benzene From Allybenzene By
Thermal Dehydration---------------------- 138
VII
AMPHETAMINE SYNTHESES
Chapter Page
Propenylbenzenes From Allybenzene By Use
of Potassium Hydroxide-------------------- 139
Para-substituted Propenyl benzenes From
Para-substituted Benzenes; Quelet Reaction- 140
Preparation of Phenyl-1- Propanols Using the
Grignard Reagent------------------------- 142
Phenyl-1- Propanol by Reduction of
Propiophenone---------------------------- 145
4-Unsubstituted Propenyl benzenes
From 4-Methoxypropenylbenzenes----------- 146
18 Preparation of Cinnamic Acids
Cinnamic Acids from Coumarins------------ 147
Naturally occurring Coumarins------------- 148
Methyl-(alpha-methyl-styryl)-Ketone From
Benzaldehyde and MEK;
Crossed Aldol Condensation---------------- 150
alpha-Methyl-Cinnamic Acids From
Methyl-(alpha-methyl-styryl )-Ketone
Haloform Reaction------------------------ 151
alpha-Methyl-Cinnamic Acid from
Benzaldehyde----------------------------- 152
Hydrocinnamic Acid from Propiophenone----- 153
19 Preparation of Nitroalkanes
From Alkanes----------------------------- 155
Nitroalkane Producing Apparatus---'-------- 156
Preparation of Nitroethane----------------- 159
20 Separation of Optical I somers
Discovery of Optical Activity
and Stereochemistry---------------------- 160
The Stereochemistry of Amphetamine------- 161
VIII
AMPHETAMINE SYNTHESES
Chapter Page
Chirality-------------------------------- 162
Separation of d-Phenylpropanolamine------- 163
21 Para-Bromination of Substituted
Phenylalk:ylamines
4-Bromo-Phenylalkylamine Hydrobromide
Salt From Phenylalkylamines--------------- 164
Precipitation and Purification of 4-Bromo
Substituted Phenylalkylamine HBr---------- 165
4-Para-Chlorination of Phenylalkylamines--- 165
22 Hallucinogenic Drugs, Serotonin Receptors,
Dopamine and NeurotoHicity-------------- 167
Serotonin Neurotoxins--------------------- 168
Preparation of Neurotransmitters &
Neurotoxins------------------------------ 169
23 An EHcitotoHic Cause of AnHiety----------- 173
24 The Brain-------------------------------- 177
Conclusion-Renaissance of Brain Research- 179
The Quest for the Endogenous Psychotogens
of Mental IIlness-------------------------- 179
Transmethylation Theory of Schizophrenia--- 180
Tardive Dyskinesia------------------------ 181
Dopamine Hypothesis of Schizophrenia------ 182
Treatment of 'Symptoms' Can Be Dangerous-- 186
S-Adenosylmethionine--------------------- 188
Those factors which Are Considered in the
Recovery of Those with out the Use of Drugs- 188
Scientific Inquiry------------------------ 189
LD-50's of Conuentional Psychoactiues---- 193
References------------------------------ 200
IndeH----------------------------------- 237
IX