| 摘要 |
Propargyl glycine derivatives of formula (I), and their racemates, enantiomers, and mixtures, are new. R2 = propargyl (CH2C?=CH) or a group CH2C?=C-Het; Het = 2-aminopyridyl, 2-amino-pyrimidyl, 6-amino-pyridazinyl (all 3 optionally substituted by 1-4C alkyl) or 4-imidazolyl (optionally substituted on positions 2 and/or 5 by 1-4C alkyl, and on position 1 or 3 by a protecting group such as trityl, benzenesulphonyl, toluenesulphonyl or dimethylaminosulphonyl); R3, R4 = H, 1-4C alkyl, 1-4C alkoxycarbonyl, ArCH2COO or ArSO2; Ar = aryl, especially 3-methyl-quinolin-8-yl or 3-methyl-1,2,3,4-tetrahydroquinolin-8-yl, or a group of formula (i); R7 = H or COR; R =1-7C alkyl, (CH2)nOCH3 or CH2O(C2H4O)nCH3; n = 1-3; A = phenyl, pyrimidyl, pyridinyl, thienyl, thiazolyl or furyl (all optionally substituted by one or more halo, 1-4C alkyl, 1-4C alkoxy, CF3, formyl, CH2OR10, CH2OCOR10, CH2OCONR10R11, COOR10, CONR10R11, NO2, NR10R11 or NHCOR10; R5 = H, 1-4C alkyl, 1-4C alkoxy carbonyl, aryl or aryl(1- 4C alkyl); R6 = 1-4C alkoxy, benzyloxy or a piperidino group of formula (ii); R12 = H, carboxyl or 1-4C alkoxycarbonyl; and R13 = 1-4C alkyl. Also new are compounds of formula (III) where R6 = (ii); R12 is not H; and R4 = ArCH2CO2 or ArSO2.
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