Claims
- 1. A prostacyclin intermediate of formula IX ##STR2## wherein R.sub.28 is --OR.sub.10, --CH.sub.2 OR.sub.10, hydroxy, hydroxymethyl, or hydrogen, wherein R.sub.10 is a blocking group removable by mild acidic hydrolysis;
- wherein Y.sub.1 is
- (1) trans--CH.dbd.CH--,
- (2) cis--CH.dbd.CH--,
- (3) --CH.sub.2 CH.sub.2 --, or
- (4) --C.tbd.C--,
- wherein M.sub.8 is .alpha.-R.sub.5 :.beta.-OR.sub.10 or .alpha.-OR.sub.10 :.beta.-R.sub.5, wherein R.sub.5 is hydrogen or methyl and R.sub.10 is as defined above, or
- .alpha.-R.sub.5 :.beta.-OH or .alpha.-OH:.beta.-R.sub.5, wherein R.sub.5 is as defined above;
- wherein L.sub.1 is .alpha.-R.sub.3 :.beta.-R.sub.4, .alpha.-R.sub.4 :.beta.-R.sub.3, or a mixture of .alpha.-R.sub.3 :.beta.-R.sub.4 and .alpha.-R.sub.4 :.beta.-R.sub.3, wherein R.sub.3 and R.sub.4 are hydrogen, methyl, or fluoro, being the same or different, with the proviso that one of R.sub.3 and R.sub.4 is fluoro only when the other is hydrogen or fluoro;
- wherein R.sub.7 is
- (1) --(CH.sub.2).sub.m --CH.sub.3, wherein m is an integer from one to 5, inclusive;
- (2) phenoxy;
- (3) phenoxy substituted by one, 2 or 3 chloro, fluoro, trifluoromethyl, alkyl of one to 3 carbon atoms, inclusive, or alkoxy of one to 3 carbon atoms, inclusive, with the proviso that not more than two substituents are other than alkyl;
- (4) phenyl;
- (5) phenyl substituted by one, 2 or 3 chloro, fluoro, trifluoromethyl, alkyl of one to 3 carbon atoms, inclusive, or alkoxy of one to 3 carbon atoms, inclusive, with the proviso that not more than two substituents are other than alkyl;
- (6) phenylmethyl, phenylethyl, or phenylpropyl; or
- (7) phenylmethyl, phenylethyl, or phenylpropyl substituted by one, 2 or 3 chloro, fluoro, trifluoromethyl, alkyl of one to 3 carbon atoms, inclusive, or alkoxy of one to 3 carbon atoms, inclusive, with the proviso that not more than two substituents are other than alkyl; with the proviso that R.sub.7 is phenoxy or substituted phenoxy, only when R.sub.3 and R.sub.4 are hydrogen or methyl, being the same or different;
- wherein R.sub.1 is
- (1) hydrogen;
- (2) alkyl of one to 12 carbon atoms, inclusive;
- (3) cycloalkyl of 3 to 10 carbon atoms, inclusive;
- (4) aralkyl of 7 to 12 carbon atoms, inclusive;
- (5) phenyl;
- (6) phenyl substituted with one, 2 or 3 chloro or alkyl of one to 3 carbon atoms; or
- (7) phenyl substituted in the para position by
- (a) --NH--CO--R.sub.25
- (b) --CO--R.sub.26
- (c) --O--CO--R.sub.27
- (d) --CH.dbd.N--NH--CO--NH.sub.2
- wherein R.sub.25 is methyl, phenyl, acetamidophenyl, benzamidophenyl, or --NH.sub.2 ; R.sub.26 is hydroxy, methyl, phenyl, --NH.sub.2, or methoxy; and R.sub.27 is phenyl or acetamidophenyl, inclusive, or a pharmacologically acceptable salt thereof when R.sub.1 is hydrogen.
CROSS REFERENCE TO RELATED APPLICATION
This application is a division of Ser. No. 062,443, now U.S. Pat. No. 4,312,810 filed July 31, 1979, which is a continuation-in-part of Ser. No. 962,845, filed Nov. 22, 1978, now abandoned.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
4123441 |
Johnson |
Oct 1978 |
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Divisions (1)
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Number |
Date |
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Parent |
62443 |
Jul 1979 |
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Continuation in Parts (1)
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Number |
Date |
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962845 |
Nov 1978 |
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