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    • 3. 发明申请
    • PROCESS FOR PRODUCING 6(R)-[2-(8'(S)-2
    • 生产6(R) - [2-(8'(S)-2',2“ - 二甲基丁酰氧基-2'(S),6'(R) - 二甲基-1,2,6,7',8 ',8A'(R) - 六氢萘-2-基](S))乙基] -4(R) - 羟基-3,4,5,6-四氢-2H-吡喃-2-酮
    • WO2009013764A2
    • 2009-01-29
    • PCT/IN2008/000467
    • 2008-07-24
    • JUBILANT ORGANOSYS LIMITEDSINGH, HarnamDUBEY, Shailendra KumarGUPTA, NitinDUBEY, Sushil Kumar
    • SINGH, HarnamDUBEY, Shailendra KumarGUPTA, NitinDUBEY, Sushil Kumar
    • C07D309/30
    • Disclosed herein is an improved process for producing HMG-CoA reductase inhibitor, 6(R)-[2-(8 '(S)-2 ",2 ''-dimethylbutyryloxy-2'(S),6 '(R)-dimethyl- 1', 2', 6', 7', 8',8a'(R)-hexahydronaphthyl-r(S))ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H- pyran-2-one, the process comprising hydrolyzing (lS,3R,7S,8S,8aR)-8-{2-[(2R,4R)- 4-hydroxy-6-oxotetrahydro-2H-ρyran-2-yl]ethyl}-3,7-dimethyl-l,2,3,7,8,8a- hexahydronaphthalen-1-yl (2S)-2-methylbutanoate in presence of a base and antioxidant, lactonizing and selectively protecting the hydroxyl group of the resultant compound, followed by acylation with an acylating agent to obtain 6(R)-[2-(8'(S)- 2",2''-dimethylbutyryloxy-2 '(S),6 '(R)-dimethyl- 1',2',6',7',8',8a'(R)- hexahydronaphthyl-r(S))ethyl]-4(R)-substituted)-3,4,5,6-tetrahydro-2H-pyran-2-one and further deprotection to obtain 6(R)-[2-(8'(S)-2",2"-dimethylbutyryloxy- 2'(S),6'(R)-dimethyl-1',2',6',7',8',8a'(R)-hexahydronaphthyl-1'(S))ethyl]-4(R)- hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one.
    • 本文公开了用于制备HMG-CoA还原酶抑制剂6(R) - [2-(8'(S)-2“,2” - 二甲基丁酰氧基-2'( S),6'(R) - 二甲基-1',2',6',7',8',8a'(R) - 六氢萘基-r(S))乙基] -4(R) - 羟基-3 (1S,3R,7S,8S,8aR)-8- {2 - [(2R,4R)-4-羟基-6,7-二氢-5H-吡咯并[2,3-b] - 氧代四氢-2H-吡喃-2-基]乙基} -3,7-二甲基-1,2,3,7,8,8a-六氢萘-1-基(2S)-2-甲基丁酸酯和 得到6(R) - [2-(8'(S)-2',2“ - 二甲基丁酰氧基-2'(2',3”,4'-二叔丁基二甲基甲硅烷基)氨基甲酸酯),并将其与酰化剂酰化, (R) - 二甲基-1',2',6',7',8',8a'(R) - 六氢萘基-r(S))乙基] -4(R) - 取代的) - (S)-2“,2” - 二甲基丁酰氧基-2'(S)-2 - [(2R) (R) - 二甲基-1',2',6',7',8',8a'(R) - 六氢萘基-1'(S))乙基] -4(R) - 羟基-3' 4,5 ,6-四氢-2H-吡喃-2-酮