Oxy-alkylamino acids and esters

Details Oxy-alkylamino acids and esters Oxy-alkylamino acids and esters

1978-11-22

1980-05-06

Helfin, Bernard

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

560 21, 560 22, 560121, 560125, 560156, 560170, 560250, 560253, 560254, 560255, 562435, 562437, 562444, 562503, 562507, 562564, 562568, C07C10120

Patent

active

042018641

ABSTRACT:
Compounds of formula (I): ##STR1## wherein: m is 1 or 2; n is 4 to 8; X is CO, protected CO, or CROH wherein R is hydrogen or C.sub.1-4 alkyl and wherein the OH moiety may be protected; R.sub.1 is hydrogen or CO.sub.2 R.sub.1 represents an ester group in which the R.sub.1 moiety contains from 1 to 12 carbon atoms; R.sub.3 is hydroxy, or protected hydroxy; R.sub.2 and R.sub.4 are separately hydrogen, C.sub.1-9 alkyl, C.sub.5-8 cycloalkyl, C.sub.5-8 cycloalkyl-C.sub.1-6 alkyl, phenyl, phenyl C.sub.1-6 alkyl, naphthyl, naphthyl C.sub.1-6 alkyl, any of which phenyl or naphthyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or nitro groups; or R.sub.2 and R.sub.4 taken with the carbon atom to which they are joined represent a C.sub.5-8 cycloalkyl group; and salts thereof; except that when one of R.sub.2 and R.sub.4 is hydrogen or C.sub.1-4 alkyl then the other of R.sub.2 and R.sub.4 cannot be hydrogen or C.sub.1-9 alkyl; have useful pharmacological properties including antigastric secretion, bronchodilator and platelet aggregration inhibition activities.

REFERENCES:
patent: 2582257 (1952-01-01), Jones
patent: 3873566 (1975-03-01), Seribner
Tancheck et al., Chem. Absts., 81, 136 472(k) (1974).
Singerman et al., Chem. Absts., 65, 5523(b) (1966).
Cassidy et al., Chem. Absts., 85, 192576(s) 1976.
Bolliger et al. Tet. Letters, 2931 (1975).

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