AMPHETAMINE

SYNTHESES

OVERVIEW
&
REFERENCE GUIDE FOR
PROFESSIONALS

by OTTO SNOW

PSYCHOACTIVE
SYNTHESIS SERIES
VOLUME 1
 AMPHETAMINE SYNTHESES

TflBLE OF CONTENTS
Chapter Page

Dedication iii
Reader's Notice x
Introduction xi
1 Psychopharmaceutical Trade 1
2 The History of Psychoactiue Chemistry 7
3 Designer Drugs 13
Controlled Substance Analogue Act 21
4 The TUJO Prong flttack -: 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, Methylarhphetamine
& Substituted Phenylisopropylamines 52
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 AMPHETAMINE SYNTHESES

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Ephedrine Alkaloids--- 58
Aminoketones; Cathinones 61
8 Reductions 63
Reduction of Phenyl-2-propanone Using
Aluminum Amalgam and Amine Solution 63
Reduction of Phenyl-2-propanone Using
Aluminum Turnings, Mercuric Bichloride
and Amine Solution 64
Reduction of Phenyl-2-propanone Using
Aluminum Amalgam with Nitroalkane 65
Phenylethylamines from fc-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
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Phenyl-2-nitropropenes From
Pseudonitrosites 85
1 -(Phenyl)-l -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-1,2-Propanediol Diacetates
From Propenylbenzenes 93
P-2-P From Phenyl-1,2-Propanediol
Diacetates 94
Friedel-Crafts Reaction; Ketones From Phenols 94
11 Preparation of Rlpha-Methylphenylalanines
From Phenyl-2-Propanones 96
12 Rmohetamines From
Phenylisopropyl-N-Formamides 100
Phenylisopropyl-N-Formamides From:
(A) Leuckart-Wallach Reaction;
P-2-P and Ammonium Formate 102
(B) 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: fc-Phenylpropionamide
from various Starting Molecules 107
Hofmann Reaction: Amphetamine from
alpha-Methyl-Phenylpropionamide 108
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13 Rmphetamines From
Phenyl-2-Bromopropane 110
Phenyl-2-Bromopropane from Allybenzenes— 111
14 Norpseudoephedrine (Kathine) From
Phenylprooanolamine— -r— 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 Phenylorooenes 130
Ally and propenylbenzenes from
Natural Sources • 130
Propenylbenzenes From Phenyl-1-Propanols- 136
Allybenzene From 3-Phenyl-1-propanol By
Thermal Dehydration 137
Propenylbenzene From Allybenzene By
Thermal Dehydration 138
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Propenylbenzenes From Allybenzene By Use

of Potassium Hydroxide 139
Para-substituted Propenylbenzenes 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 Propenylbenzenes
From 4-Methoxypropenylbenzenes 146
18 Preparation of Cinnamic Reids
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 Isomers
Discovery of Optical Activity
and Stereochemistry 160
The Stereochemistry of Amphetamine 161
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Chirality 162
Separation of d-Phenylpropanolamine 163
21 Para-Bromination of Substituted
Phenylalkylamines
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.
Dooamine and NeurotoKicity 167
Serotonin Neurotoxins 168
Preparation of Neurotransmitters &
Neurotoxins 169
23 Rn EncitotoHic Cause of Rnniety 173
24 The Brain 177
Conclusion-Renaissance of Brain Research- 179
The Quest for the Endogenous Psychotogens
of Mental Illness 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
Inden 237
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