| 摘要 |
1323179 Benzopyran derivatives TROPON GmbH [trading as TROPONWERKE DINKLAGE & CO] 16 July 1971 [17 July 1970 20 Feb 1971] 33525/71 Heading C2C The invention comprises novel benzopyran derivatives of the formula in which R 1 , R 2 , R 5 and R 6 each are H, C 1-4 alkyl, cycloalkyl, aralkyl or aryl, or R 1 and R 2 , and/or R 5 and R 6 together with the adjacent nitrogen atom form a saturated heterocyclic ring containing 3 to 7 ring members of which 1 to 3 can be hetero atoms; R 4 is H or C 1-3 alkyl; R 7 is H, C 1-3 alkyl or aryl; Z is halogen, C 1-3 alkyl or C 1-3 alkoxy; n is 0 to 2; and U is C 2-5 alkylene optionally substituted by a hydroxyl group, and acid addition salts thereof. The compounds are prepared by reacting amines of the formula HN(R 1 )R 2 or HN(R 5 )R 6 with compounds of the formulµ wherein R 8 is alkyl or aryl, Hal is halogen, and R 9 and R 10 have the same meanings as R 1 and R 2 , provided the radical -NR 9 R 10 is not identical to -N(R 5 )R 6 . Alternatively, the compounds may be prepared by reacting the appropriate 7-amino (or 7-alkylamino)-3,4-disubstituted - 2 - oxo - 2H - 1 - benzo - pyran with isocyanates of the formula R 5 -NCO, or with compounds of the formula Hal-CO-N(R 5 )R 6 or with compounds of the formula N#C-N (R 5 )R 6 , followed by hydrolysis of the resulting guanidine derivative. Phenyl and ethyl N-[3-(2-chloroethyl)-4-methyl- 2 - oxo - 2H - 1 - benzopyran - 7 - yl]carbamates are obtained by reacting 2-acetyl-Y-butyrolactone with phenyl and ethyl N-(3-hydroxyphenyl)carbamates. N - Methyl - N - [3 - (2 - morpholinoethyl)-4- methyl - 2 - oxo - 2H - 1 - benzopyran - 7 - yl] carbamoyl chloride is obtained by reacting phosgene with 7-methylamino-3-(2-morpholinoethyl) - 4 - methyl - 2 - oxo - 1H - 1 - benzopyran. Pharmaceutical compositions suitable for oral, parenteral or rectal administration contain the above novel benzopyran derivatives or acid addition salts thereof and carriers therefor. The compounds coronary-dilating activity.
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