Enzyme-catalyzed asymmetric deacylation for the preparation of lasofoxifene (CP-336156), a selective estrogen receptor modulator

被引:20
作者
Yang, XJ [1 ]
Reinhold, AR [1 ]
Rosati, RL [1 ]
Liu, KKC [1 ]
机构
[1] Pfizer Inc, Cent Res, Groton, CT 06340 USA
关键词
D O I
10.1021/ol006652+
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A potent and selective estrogen receptor modulator (SERM), Lasofoxifene (CP-336156), was prepared by an enzyme-catalyzed asymmetric deacylation with high optical purity and excellent yield even though the hydrolytic site is remote from the chiral centers.
引用
收藏
页码:4025 / 4027
页数:3
相关论文
共 30 条
  • [1] Selective estrogen receptor modulators (SERMs): Effects on multiple organ systems
    Agnusdei, D
    Lori, N
    [J]. CURRENT MEDICINAL CHEMISTRY, 2000, 7 (05) : 577 - 584
  • [2] RALOXIFENE (LY139481 HCL) PREVENTS BONE LOSS AND REDUCES SERUM-CHOLESTEROL WITHOUT CAUSING UTERINE HYPERTROPHY IN OVARIECTOMIZED RATS
    BLACK, LJ
    SATO, M
    ROWLEY, ER
    MAGEE, DE
    BEKELE, A
    WILLIAMS, DC
    CULLINAN, GJ
    BENDELE, R
    KAUFFMAN, RF
    BENSCH, WR
    FROLIK, CA
    TERMINE, JD
    BRYANT, HU
    [J]. JOURNAL OF CLINICAL INVESTIGATION, 1994, 93 (01) : 63 - 69
  • [3] Cameron K. O., Patents JP, Patent No. 98503215
  • [4] Cameron K. O., Patents US, Patent No. 5552412
  • [5] Cameron K. O., Patents WO, Patent No. [WO/96/21656 A1, 9621656]
  • [6] Cameron K. O., Patents EP, Patent No. 802910
  • [7] Carnell AJ, 1999, ANN R C ORG, V95, P39, DOI 10.1039/a808596j
  • [8] QUANTITATIVE-ANALYSES OF BIOCHEMICAL KINETIC RESOLUTIONS OF ENANTIOMERS
    CHEN, CS
    FUJIMOTO, Y
    GIRDAUKAS, G
    SIH, CJ
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1982, 104 (25) : 7294 - 7299
  • [9] Chiu CK, PCT Int. Appl, Patent No. [WO/97/16434 A1, 9716434]
  • [10] Drauz K., 1995, ENZYME CATALYSIS ORG