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    • 7. 发明公开
    • Synthesis of intermediates for the preparation of pramipexol
    • Herstellung von Pramipexol的Synthese von Zwischenproduktenfürdie
    • EP1808492A1
    • 2007-07-18
    • EP07000277.9
    • 2007-01-08
    • Dipharma Francis S.r.l.
    • Riva, SergioFassi, PaolaScarpellini, MicheleAllegrini, PietroRazzetti, Gabriele
    • C12P17/14C12P41/00C07D277/82
    • C12P17/14C07D277/82C12P41/005
    • A process for the preparation of an acid of formula (I), as the individual (R) enantiomer or (S), or a salt thereof

      wherein R is a protected amino group; and the asterisk * denotes the stereogenic carbon atom, comprising contacting an ester of formula (II), as mixture of (R,S) enantiomers, or a salt thereof,

      wherein R 1 is straight or branched C 1 -C 6 alkyl, optionally substituted with phenyl; and the asterisk * and R have the meanings defined above, with a lipase from Candida antarctica, under conditions effective to obtain a mixture comprising an acid of formula (I), as the individual (R) enantiomer, and an ester of formula (II), as the individual (S) enantiomer; the subsequent hydrolysis of the latter to obtain an acid of formula (I), as the individual (S) enantiomer; and, if desired, the conversion of an acid of formula (I), either as the (R) or (S) enantiomer, to a salt thereof.
    • 制备式(I)的酸作为单独的(R)对映异构体或(S)的酸的方法或其盐,其中R是被保护的氨基; 并且星号*表示立体碳原子,包括使式(II)的酯作为(R,S)对映异构体或其盐的混合物,其中R 1是直链或支链C 1 -C 6烷基,任选地 被苯基取代; 和星号*和R具有上述定义,与来自南极念珠菌的脂肪酶在有效获得包含式(I)的酸的混合物作为单独的(R)对映体的条件下,和式(II)的酯 ),作为个体(S)对映异构体; 随后水解后者以获得式(I)的酸作为个体(S)对映异构体; 如果需要,将式(I)的酸作为(R)或(S)对映异构体转化为其盐。
    • 10. 发明公开
    • Process for preparing optically active benzothiazepine compound, and intermediate therefor
    • 一种制备光学活性的苯并硫氮杂化合物和中间体为此过程
    • EP0826678A1
    • 1998-03-04
    • EP97114700.4
    • 1997-08-25
    • TANABE SEIYAKU CO., LTD.
    • Kometani, TadashiMatsumae, HiroakiShibatani, Takeji
    • C07D281/10C12P17/14
    • C07D281/10C12P17/14
    • Powdery aggregate of 2-phenyl-1,5-benzothiazepin-3,4(2H,5H)-dione compound:
      wherein Ring A and Ring B are benzene ring having optionally substituent selected from lower alkyl, lower alkoxy and halogen, which is prepared by admixing solution of the compound (II) in polar organic solvent with solvent which does not substantially dissolve the compound (II) but is miscible with said polar organic solvent, and separating and collecting the resultant particles of the compound (II). Said aggregate of the compound (II) can be converted into optically active 3-hydroxy-2-phenyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one compounds (I) on industrial scale, which are useful as intermediate for various medicaments.
    • 2-苯基-1,5-苯并硫氮杂-3,4(2H,5H) - 二酮化合物的粉末状集聚体: worin环A和环B是任选具有取代基选自低级烷基,低级烷氧基和卤素的苯环, 所有这些是通过混合在极性有机溶剂中的化合物(II)的溶液用溶剂基本上不溶解化合物(II),但是可混溶的与所述极性有机溶剂,并分离和收集所得颗粒中的化合物的制备(II) , 所述化合物(II)的聚集体可以在工业规模上,这是被转换成光学活性的3-羟基-2-苯基-2,3-二氢-1,5-苯并硫氮杂-4(5H) - 酮化合物(I) 可用作中间体的各种药物。