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    • 8. 发明申请
    • PROCESS FOR PRODUCING 6(R)-[2-(8'(S)-2
    • 制备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) - 十六氢萘基-L'(S))乙基] -4(R) - 羟基-3,4,5,6-四氢-2H-吡喃-2-酮
    • WO2009013764A3
    • 2009-03-19
    • PCT/IN2008000467
    • 2008-07-24
    • JUBILANT ORGANOSYS LTDSINGH HARNAMDUBEY SHAILENDRA KUMARGUPTA NITINDUBEY SUSHIL KUMAR
    • SINGH HARNAMDUBEY SHAILENDRA KUMARGUPTA NITINDUBEY SUSHIL KUMAR
    • C07D309/30
    • 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-?yran-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.
    • 本文公开了一种生产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) - (R) - 六氢萘基-r(S))乙基] -4(R) - 羟基-3,4,5,6-四氢 - (1S,3R,7S,8S,8aR)-8- {2 - [(2R,4R)-4-羟基-6-氧代四氢-2H-哒嗪-2 - 基]乙基} -3,7-二甲基-1,2,3,7,8,8a-六氢萘-1-基(2S)-2-甲基丁酸酯在碱和抗氧化剂存在下,内酯化和选择性保护羟基 然后用酰化剂酰化,得到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) - 取代的) 四氢-2H-吡喃-2-酮,进一步脱保护,得到6(R) - [2-(8'(S)-2“,2” - 二甲基丁酰氧基-2'(S),6'(R) -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。