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    • 3. 发明授权
    • Process for the purification or isolation of
(2S,3R)-1-halo-2-hydroxy-3-(protected amino)4-phenylthiobutanes or
optical antipodes thereof
    • 纯化或分离(2S,3R)-1-卤代-2-羟基-3-(被保护的氨基)-4-苯硫基丁烷或其光学对映体的方法
    • US6107511A
    • 2000-08-22
    • US269298
    • 1999-05-14
    • Yasuyoshi UedaKatsuji MaeharaTadashi SugawaHiroshi MuraoAkira NishiyamaHajime Manabe
    • Yasuyoshi UedaKatsuji MaeharaTadashi SugawaHiroshi MuraoAkira NishiyamaHajime Manabe
    • C07C319/28C07C323/43C07C261/00
    • C07C319/28Y02P20/55
    • The present invention has for its object to provide a commercially useful, expedient and efficient method for purification and isolation of an N-protected (2S,3R)-1-halo-2-hydroxy-3-amino-4-phenylthiobutane (1) or its enantiomer, which is capable of removing the various contaminants, particularly said byproducts, whereby the problem of instability of the compound (1) or its enantiomer can be overcome and a high product yield can be insured.The present invention relates to a method of purifying and isolating an N-protected (2S,3R)-1-halo-2-hydroxy-3-amino-4-phenylthiobutane (1): ##STR1## (wherein X represents a halogen atom; one of P.sup.1 and P.sup.2 represents a hydrogen atom and the other represents an amino-protecting group, or P.sup.1 and P.sup.2 taken together represents an amino-protecting group) or its enantiomer, which comprises using an aromatic hydrocarbon solvent to remove impurities occurring in said compound (1) or impurities occurring in said enantiomer from said compound (1) containing impurities or its enantiomer containing impurities and isolate said compound (1) or said enantiomer as crystals.
    • PCT No.PCT / JP98 / 03375 Sec。 371日期1999年5月14日 102(e)日期1999年5月14日PCT提交1998年7月29日PCT公布。 出版物WO99 /​​ 06364 日期1999年2月11日本发明的目的是提供用于纯化和分离N-保护的(2S,3R)-1-卤代-2-羟基-3-氨基-4 (1)或其对映异构体,其能够除去各种污染物,特别是所述副产物,由此可以克服化合物(1)或其对映体的不稳定性问题,并且可以保证高产率。 本发明涉及纯化和分离N-保护的(2S,3R)-1-卤代-2-羟基-3-氨基-4-苯基硫代丁烷(1)的方法:(其中X表示卤素原子; P1和P2表示氢原子,另一个表示氨基保护基,或P1和P2一起表示氨基保护基)或其对映异构体,其包括使用芳烃溶剂除去在所述化合物(1)中发生的杂质 )或杂质存在于所述含有杂质的化合物(1)的所述对映异构体中,或将所述化合物(1)或所述对映异构体分离为晶体。