Intermediates for producing 9-substituted carbacyclin analogs

Details Intermediates for producing 9-substituted carbacyclin analogs Intermediates for producing 9-substituted carbacyclin analogs

C - Chemistry, Metallurgy

07

F

260/235.01

C07F 7/08 (2006.01) C07D 333/24 (2006.01) C07C 177/00 (1985.01)

Patent

CA 1228588

ABSTRACT Intermediates for preparing 9-substituted carbacyclin analogs of general formula: Image (Va) or Image (IXa/Xa) wherein s is one or 2; D is cis-?=C(R3)-, trans-?=C(R3) or Image ; wherein R3 is H or F; R21 is a silyl-protected group of general formula Si(G1)3, wherein G1 is a conventional silyl-protecting group; R50 is Cl, I, -CF3 or -COOH; Y is cis-CH=CH-, trans-CH=CH-, -CH2CH2- or -C?C-; Z is (i) trans-CH2-CH=CH-, (ii) -CH2-(CH2)f-C(R4)2-, wherein f is zero, one, 2 or 3 and each R4 is the same and is a group selected from H and F, or (iii) when R3 is H, -(Ph)-(CH2)g-, wherein g is zero, one, 2 or 3 and Pn is 1,2-, 1,3- or 1,4-phenylene; Lx is H:H,.alpha.-OR?2:.beta.-H, .alpha.-H:.beta.-OR?2, .alpha.-CH2OR?2:.beta.-H or .alpha.-H:.beta.-CH2OR?2, wherein R?2 is an -OH-protecting group; Mx is .alpha.-OR?2:.beta.-R14 or .alpha.-R14:.beta.-OR?2, wherein R?2 is as defined above and R14 is H or -CH3; L1 is .alpha.-R15:.beta.-R16, .alpha.-R16:.beta.-R15 or a mixture thereof, wherein R15 and R16, independently are H, F or -CH3, with the proviso that one of R15 and R16 is F only when the other is not -CH3; and R17 is (iv) cis-CH=CHCH2CH3, -(CH2)2CH(OH)CH3, -(CH2)3CH=C(CH3)2, Image , phenyl, benzyl, phenylethyl, phenylpropyl, Image and Image , (v) -CmH2mCH3, wherein m is an integer of from one to 5, or (vi) mono-, di- and tri-F, -C1, -CF3, -C1-3alkyl and -C1-3alkoxy-( ring )-substituted-phenyl, -benzyl, -phenylethyl or -phenylpropyl, with the proviso that not more than two substituents are other than C1-3alkyl; or Image , when taken together, is (vii) Image , 3-thienyloxymethyl, C4-7cycloalkyl or mono- di- and tri-C1-5alkyl-substituted C4-7cycloalkyl, (viii) -C?CCqH2qCH3, wherein q is an integer of from 2 to 6, or (ix) -CpH2 CH=CH2, wherein p is an integer of from 3 to 7.

485771

Affiliated with

Also associated with

Rating

Intermediates for producing 9-substituted carbacyclin analogs does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Intermediates for producing 9-substituted carbacyclin analogs, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Intermediates for producing 9-substituted carbacyclin analogs will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-1188217