CO-NH2 CO-NH2 â€žâ€žCO-NH2 CO-NH2

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4 INTRODUCTION Eventually the field was expanded, and interesting antihistaminics, parasympatholytics and analgesics (e.g. Actidyl*, Akineton*, Amolanone, bromprophenpyridamine, chlorprophenpyridamine, cycrimine, hexocyclium, mepiperphenidol, Par KS 12, piperphenidol, procyclidine, prophenpyridamine, propoxyphene, pyrrobutamine, Spalisal*, thiambutene, tricyclamol, tridihexethide iodide and trihexyphenidyl) were developed by changing the basic side chain or the phenyl rings of structure (I).
CHAPTER I A n a l g e s i c " Activity i n M a n a n d in A n i m a l s A <strong>CO</strong>MPOUND is said to possess "analgesic" activity when it is capable of relieving pain. Pain, of course, is a universal subjective experience of mankind, and everybody knows what is meant by it (39) . Hence there is no point in trying to define this basic concept. In man, pain can be evoked by various "noxious" stimuli, such as heat, pressure, chemicals, electric current, etc. When such stimuli are applied to animals, their behaviour changes in a typical way. Generally speaking the animal either tries to avoid the stimulus by various flight reactions or, when (light is made impossible, it shows a series of reflexes, which are often interpreted as signs of discomfort. In man, the evidence on whether or not pain is iclieved, is entirely based on the statement of the subject as expressed in the interview made by the observer. The nature of such statements, however, depends on several factors in constant operation, such as the willingness of (he subject to talk about his feelings, the attitude of the observer towards the subject, the influence of the environment on the subject, his immediate problems, his hope or desperation and many other factors. Obviously, therefore, the study of the influence of one single factor, such as the administration of a drug, on the statements of a given subject necessitates special techniques. The elimination of bias on the part of the subject or the observer emerges clearly as a basic and essential requirement for such studies (39) . Recently, the various problems concerning the measurement of pain and relief of pain were adequately reviewed by Beecher (39) . In view of the fact that pain is, by definition, a subjective sensation of mankind, it can, strictly speaking, only be studied in humans. What we are able to study in animals is not pain itself, but the behaviour of the animal following a stimulus which provokes pain in man and also, of course, the influence of a given factor, such as the administration of a certain drug on the reactions of the animal. Rather full lists of references to the methods of producing "pain" for experimental purposes are given by BEECHER (39) and 5
Page 1 and 2: S Y N T H E T I C A N A L G E S I C
Page 3: C o n t e n t s Page Preface . . .
Page 7 and 8: I n t r o d u c t i o n THE main pu
Page 9: 15. 16. 17. 18. 19. 20. 21. CONH2 C
Page 13 and 14: CHAPTER II T h e " A n a l g e s i
Page 15 and 16: METHADONE, MORPHINE, PETHIDINE AND
Page 17 and 18: Symbol ED50 ED50 ED50 ED50 ED50 ED5
Page 19 and 20: CHAPTER III 3 : 3 - D i p h e n y l
Page 21 and 22: o .s HI S T oo HJ * 3 :3-DIPHENYLPR
Page 23 and 24: 2.1 2.2 2.3 2.4 2.5 2.6 OH „ OH O
Page 25 and 26: 2.15 2.16 2.17 2.18 2.19 2.20 2.21
Page 27 and 28: 3.15 4.1 4.2 4.3 4.4 4.5 4.6 4-7 5.
Page 29 and 30: 5.4 5.5 „ 55 » „ CN CN „ „
Page 31 and 32: 5.14 5.15 5.16 5.17 5.18 5.19 5.20
Page 33 and 34: 5.35 5.36 5.37 5.38 5.39 5.40 5.41
Page 35 and 36: 6.9 6.10 6.11 6.12 6.13 6.14 6.15 6
Page 37 and 38: 6.46 6.47 6.48 6.49 6.50 6.51 6.52
Page 39 and 40: 7.4 7.5 7.6 7.7 7.8 7.9 7.10 7.11 C
Page 41 and 42: 7.26 7.27 7.28 7.29 7.30 7.31 7.32
Page 43 and 44: 8,15 8.16 8.17 9.1 9.2 9.3 9.4 9.5
Page 45 and 46: 10.4 1 _ CONi,CH3j, 2 H" HH N CK- N
Page 47 and 48: 10.47 10.48 10.49 10.50 10.51 10.52
Page 49 and 50: 11.15 COOC-H5 11.14 COOCHg 11.15 11
Page 51 and 52: 13.9 13.10 13.11 CH-C.H5OOC- CH3
Page 53 and 54: 13.13 13.24 13.25 13.26 13.27 13.28
Page 55 and 56: 1-*»1Z c c.:-:f XH 14.13 14.14 14.
Page 57 and 58: 14.56 14.37 14.38 14.39 COCH; COCH3
Page 59 and 60: •> 5 5? 5 5 55 M » I n 5 w 5? )?
Page 61 and 62:
14.49 14.50 14.51 14.52 14.53 14.54
Page 63 and 64:
14.66 14.67 14.68 14.69 14.70 14.71
Page 65 and 66:
14.9" CO-C£H£ 14.98 14.99 14.100
Page 67 and 68:
16.13 16.14 17.1 17.2 17.3 17.4 17.
Page 69 and 70:
ti 1.1 1.2 1.3 1.4 1.5 1.6 1.7 1.8
Page 71 and 72:
2.4 2.5 2.6 2.7 2.8 2.9 2.13 2.14 2
Page 73 and 74:
3.5 3.7 4.1 4.3 4.4 4.5 4.7 5.1 5.2
Page 75 and 76:
5.53 5.59 6.1 6.4 6.8 6.9 6.14 6.18
Page 77 and 78:
3:3-DIPHENYLPROPYLAMINES 71 flo****
Page 79 and 80:
9.19 9.20 9.21 9.22 9.23 9.26 9.27
Page 81 and 82:
10.22 10.23 10.24 10.25 10.26 10.30
Page 83 and 84:
10.42 10.43 10.59 10.60 10.61 10.62
Page 85 and 86:
11.7 11.8 11.9 11.10 11.11 11.12 11
Page 87 and 88:
„ — R- 13.10 — CF RT R- CF CF
Page 89 and 90:
13.24 13.25 13.27 13.31 13.33 13,35
Page 91 and 92:
14.36 14.37 14.38 14.39 „ RT RT R
Page 93 and 94:
CF RT CF RT ET RB •>•> PRT ET R
Page 95 and 96:
14.41 14.42 14.43 14.44 RB — CF ,
Page 97 and 98:
14.54 14.55 14.56 14.57 14.58 14.59
Page 99 and 100:
14.76 14.77 14.78 14.82 14.83 14.84
Page 101 and 102:
If o ^ 1.1 1.4 1.5 1.6 1.8 1.9 1.10
Page 103 and 104:
3.3 3.4 5.1 5.2 5.3 — — — —
Page 105 and 106:
5.6 5.9 5.12 5.13 5.17 5.27 5.32 5.
Page 107 and 108:
8.8 10.2 10.41 10.43 11.4 11.6 11.9
Page 109 and 110:
14.40 8-99 10-12 d-nci /-base /-bas
Page 111 and 112:
X 14.57 14.64 14.65 14.66 14.69 14.
Page 113 and 114:
Continued from p. 13 3 :3-DIPHENYLP
Page 115 and 116:
3:3-DIPHENYLPROPYLAMINES 109 antisp
Page 117 and 118:
TERTIARY ALCOHOLS 111 halide with a
Page 119 and 120:
TERTIARY ALCOHOLS 113 Tertiary alco
Page 121 and 122:
CHAPTER V S e c o n d a r y A l c o
Page 123 and 124:
5-3 SECONDARY ALCOHOLS 117 C2H5 r n
Page 125 and 126:
SECONDARY ALCOHOLS 119 In the wo-se
Page 127 and 128:
PRIMARY ALCOHOLS reduced (PtO-CH3OH
Page 129 and 130:
NITRILES 123 Basic propyl- and wopr
Page 131 and 132:
NITRILES 125 The following elegant
Page 133 and 134:
NITRILES 127 Nitriles of type [7.1]
Page 135 and 136:
CHAPTER VIII D i a m i n e s a n d
Page 137 and 138:
DIAMINES AND DERIVATIVES 131 Only o
Page 139 and 140:
PRIMARY AMIDES ^ ^NH—CH—CH—N'
Page 141 and 142:
PRIMARY AMIDES 135 Quaternization b
Page 143 and 144:
ACIDS AND ACID CHLORIDES 137 When h
Page 145 and 146:
CHAPTER XI S e c o n d a r y A m i
Page 147 and 148:
CHAPTER XII R 8 7 5 a n d R e l a t
Page 149 and 150:
TERTIARY AMIDES 143 The relation be
Page 151 and 152:
TERTIARY AMIDES 145 (1) In man R 87
Page 153 and 154:
ESTERS DERIVED FROM AMINO ACIDS 147
Page 155 and 156:
ESTERS DERIVED FROM AMINO ACIDS 149
Page 157 and 158:
CHAPTER XV Esters derived f r o m S
Page 159 and 160:
Nomenclature of derived isomers Mel
Page 161 and 162:
CHAPTER XVI K e t i m i n e s , A c
Page 163 and 164:
NAA'* N(CH3)2 „ 55 ?? ?5 *s 5 N(C
Page 165 and 166:
KETIMINES, ACYL KETIMINES AND KETON
Page 167 and 168:
CHAPTER XVIII S u l p h o n e s (I:
Page 169 and 170:
SULPHONES 163 According to KLENK et
Page 171 and 172:
OTHER COMPOUNDS OF STRUCTURE (I) 16
Page 173 and 174:
DISSOCIATION CONSTANTS Steric facto
Page 175 and 176:
R CONFIGURATIONAL STUDIES TABLE XVI
Page 177 and 178:
REFERENCES 1 ADAMI E. and MARAZZI E
Page 179 and 180:
REFERENCES 173 89 CHEN K. K. (1948)
Page 181 and 182:
REFERENCES 175 163 FRIEBEL H. and R
Page 183 and 184:
REFERENCES 177 249 KEATS A. S. and
Page 185 and 186:
REFERENCES 179 339 MOFFETT R. B. (1
Page 187 and 188:
REFERENCES 181 411 SCHULTZ E. M., R
Page 189:
REFERENCES 183 499 WHEATLEY W. B.,
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CO-NH2 CO-NH2 â€žâ€žCO-NH2 CO-NH2

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