Preparation of 19-Nor-vitamin D compounds
First Claim
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1. A 20-epi-19-nor-vitamin D compound having the structure:
- where each of X1 and X2, independently represents hydrogen or a hydroxy-protecting group, and where R is represented by the structure;
##STR14## where Z is selected from Y, --OY, --CH2 OY, --C.tbd.CY and --CH═
CHY, where the double bond may have the cis or trans stereochemical configuration, and where Y is selected from hydrogen, methyl, --CR5 O and a radical of the structure;
##STR15## where m and n, independently, represent integers from 0 to 5, where R1 is selected from hydrogen, hydroxy, protected hydroxy, fluoro, trifluoromethyl, and C1-5 -alkyl, which may be straight chain or branched and, optionally, bear a hydroxy or protected-hydroxy substituent, and where each of R2, R3, and R4, independently is selected from hydrogen, fluoro, trifluoromethyl and C1-5 -alkyl, which may be straight-chain or branched, and optionally, bear a hydroxy or protected-hydroxy substituent, and where R1 and R2, taken together, represent an oxo group, or an alkylidene group, ═
CR2 R3, or the group --(CH2)p --, where p is an integer from 2 to 5, and where R3 and R4, taken together represent an oxo group, or the group --(CH2)q --, where q is an integer from 2 to 5, and where R5 represents hydrogen, hydroxy, protected hydroxy, or C1-5 alkyl.
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Abstract
Disclosed are 20-epi-19-nor-vitamin D compounds having the structure: ##STR1## where each of X1 and X2 independently represents hydrogen or a hydroxy-protecting group, and Z represents various known side chains.
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Citations
1 Claim
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1. A 20-epi-19-nor-vitamin D compound having the structure:
where each of X1 and X2, independently represents hydrogen or a hydroxy-protecting group, and where R is represented by the structure;
##STR14## where Z is selected from Y, --OY, --CH2 OY, --C.tbd.CY and --CH═
CHY, where the double bond may have the cis or trans stereochemical configuration, and where Y is selected from hydrogen, methyl, --CR5 O and a radical of the structure;
##STR15## where m and n, independently, represent integers from 0 to 5, where R1 is selected from hydrogen, hydroxy, protected hydroxy, fluoro, trifluoromethyl, and C1-5 -alkyl, which may be straight chain or branched and, optionally, bear a hydroxy or protected-hydroxy substituent, and where each of R2, R3, and R4, independently is selected from hydrogen, fluoro, trifluoromethyl and C1-5 -alkyl, which may be straight-chain or branched, and optionally, bear a hydroxy or protected-hydroxy substituent, and where R1 and R2, taken together, represent an oxo group, or an alkylidene group, ═
CR2 R3, or the group --(CH2)p --, where p is an integer from 2 to 5, and where R3 and R4, taken together represent an oxo group, or the group --(CH2)q --, where q is an integer from 2 to 5, and where R5 represents hydrogen, hydroxy, protected hydroxy, or C1-5 alkyl.
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Current AssigneeWisconsin Alumni Research Foundation (University of Wisconsin System)
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Original AssigneeWisconsin Alumni Research Foundation (University of Wisconsin System)
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InventorsDeluca, Hector F., Aria, Fariba, Schnoes, Heinrich K.
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Primary Examiner(s)Dees, Jose G.
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Assistant Examiner(s)PRYOR, ALTON NATHANIEL
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Application NumberUS08/797,001Time in Patent Office697 DaysField of Search552/653US Class Current552/653CPC Class CodesC07C 401/00 Irradiation products of cho...C07F 7/1804 Compounds having Si-O-C lin...Y02P 20/55 Design of synthesis routes,...
