| 摘要 |
1463367 Benzhydryl/2-azacycloalkylmethyl ketones and carbinols RICHARDSON-MERRELL Inc 22 April 1974 [25 April 1973] 17547/74 Heading C2C The invention comprises compounds of formula and their pharmaceutically acceptable acid addition salts, wherein Y is O = or m=1-3, n = 3-5 and p=1-2; R 1 , R 2 and R 3 are each H or C 1-4 alkyl, and additionally R 3 may be halogen or C 1-4 alkoxy or alkylthio. The ketones are prepared by reacting a solution of the corresponding benzhydryl/methyl ketone with excess magnesium methyl carbonate, cooling and reacting the solution (which apparently contains the magnesium chelate of a 3 - benzhydryl - 3 - hydroxypropenoic acid) in a CO 2 atmosphere with a 1-azacycloalkene, and may be reduced with NaBH 4 to the alcohols. Starting materials exemplified are PhCH(Br)Ac and 2,5-Me 2 C 6 H 3 CH(Ph)Ac. Therapeutic compositions having anticoagulant activity comprise compounds of the above formula, and may be administered orally, sublingually, intrabuccally or parenterally.
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