SYNTHETICANALGESICSPART IDiphenylpropylamines
By
Paul A. J. Janssen
Research LaboratoriaDr. C. Janssen n.v, BeerseBelgiumPERGAMON PRESSNEW YORK • OXFORD • LONDON • PARIS1960
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Contents
Page
Preface ........... viiIntroduction .......... 1I "Analgesic" activity in man and in animals ..... 5LI The "analgesic" activity of methadone, morphine, pethidine and codeinein animals .......... 7III 3:3-Diphenylpropylamines (I : R = H) 13IV Tertiary alcohols (I : R = OH) 110V Secondary alcohols (I : R = CHOH alk) 115VI Primary alcohols [I : R - (CH
2
)
n
—OH;
n =
1, 2, 3] . . . .120Vll Nitriles (I : R - CN) 122VIII Diamines and derivatives (I :R contains amino group or derivative) . 129IX Primary amides (I : R = CONH
2
) 132X Acids and acid chlorides (I : R = COOH or COC1) . . . .136XI Secondary amides (I : R = CONHRO 139XII R875 and related basic tertiary amides (I : R = CONR'R") . . .141XIII Esters derived from amino acids of type I (R = COOR') . . .146XIV Esters derived from tertiary alcohols (I : R = OCOR') . . .150XV Esters derived from secondary alcohols (I : R = CHOCOR'-R') . .151XVI Ketimines, acyl ketimines and ketones (I : R = CNHR', CNCOR'-R',COR') 155XVII Aldehydes (I : R = COH) 160XVIII Sulphones (I : R = SO
2
R') 161XIX Other compounds of structure (I) . . . • . . .164XX Dissociation constants . • • . . • . . .166XXT Conflgurational studies . . . • . • • . .168References ........... 171
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