首页> 外国专利> NOVEL POLYMORPHIC FORMS OF ((1S,2S,3S,4R,5S))-2,3,4-(TRIS-BENZYLOXY)-5-(4-CHLORO- 3-(4-ETHOXY-BENZYL)PHENYL)-6,8-DIOXA-BICYCLO3.2.1OCT-1-YL-METHANOL

NOVEL POLYMORPHIC FORMS OF ((1S,2S,3S,4R,5S))-2,3,4-(TRIS-BENZYLOXY)-5-(4-CHLORO- 3-(4-ETHOXY-BENZYL)PHENYL)-6,8-DIOXA-BICYCLO3.2.1OCT-1-YL-METHANOL

机译:(((1S,2S,3S,4R,5S))-2,3,4-(三-苄基)-5-(4-氯-3-(4-乙氧基-苄基)苯基)-6的新多态形式,8-二氧杂双环[3.2.1] OCT-1-YL-甲醇

摘要

NOVEL POLYMORPHIC FORMS OF ((1S,2S,3S,4R,5S))-2,3,4-(TRIS-BENZYLOXY)-5-(4-CHLORO-3-(4-ETHOXY- BENZYL)PHENYL)-6,8-DIOXA-BICYCLO[3.2.1]OCT-1-YL-METHANOL ABSTRACT The present invention relates to novel polymorphs of ((1S,2S,3S,4R,5S))-2,3,4-(tris-benzyloxy)-5-(4-chloro-3-(4-ethoxy-benzyl)phenyl)-6,8-dioxa-bicyclo[3.2.1]oct-1-yl- methanol of formula (I) useful in the preparation of Ertugliflozin of formula (II). (I) wherein Bn refers to benzyl. The invention also relates to process for the preparation of crystalline Form G of ((1S,2S,3S,4R,5S))-2,3,4-(tris-benzyloxy)-5-(4-chloro-3-(4-ethoxy- benzyl)phenyl)-6,8-dioxa-bicyclo[3.2.1]oct-1-yl-methanol of formula (I) and characterized by X-ray powder diffraction pattern peaks selected form 5.7, 14.0, 15.6, 15.9, 17.3, 18.8, 19.7, 19.8, 23.0 ±0.2° 2. This compound of Formula I is a useful intermediate in the preparation of Ertugliflozin, which is used in the treatment of type 2 diabetes mellitus.
机译:((1S,2S,3S,4R,5S))-2,3,4-(三-苄基)-5-(4-氯-3-(4-乙氧基-苄基)苯基)-6的新多态形式本发明涉及(((1S,2S,3S,4R,5S))-2,3,4-(tris-)的新型多晶型物,8,DIOXA-BICYCLO [3.2.1] OCT-1-YL-甲醇摘要式(I)的式(I)的苄氧基)-5-(4-氯-3-(4-乙氧基-苄基)苯基)-6,8-二氧杂双环[3.2.1]辛-1-基-甲醇式(II)的艾格列净的衍生物。 (I)其中Bn是指苄基。本发明还涉及制备(((1S,2S,3S,4R,5S))-2,3,4-(三苄氧基)-5-(4-氯-3-(式(I)的4-乙氧基-苄基)苯基)-6,8-二氧杂双环[3.2.1]辛-1-基甲醇,并通过X射线粉末衍射图谱峰从5.7、14.0、15.6中选择峰进行表征,15.9、17.3、18.8、19.7、19.8、23.0±0.2°2。该式I化合物是制备Ertugliflozin的有用中间体,该药物用于治疗2型糖尿病。

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