首页> 外国专利> PROCEDURE FOR SYNTHESIZING DICLORHYDRATE SALT OF ((1S) -1 - (((2S) DICHLORHYDRATE SALT OF ((1S) -1 - (((2S) -2- (5- (4 '- (2 - ((2S) -1 - ((2S) -2 - ((METOXICARBONIL) AMINO) -3-METHYLBUTANOIL) -2-PIRROLIDINYL) -1H-IMIDAZOL-5-IL) -4-BIFENYLIL) -1H-IMIDAZOL-2-IL) - 1-PIRROLIDINIL

PROCEDURE FOR SYNTHESIZING DICLORHYDRATE SALT OF ((1S) -1 - (((2S) DICHLORHYDRATE SALT OF ((1S) -1 - (((2S) -2- (5- (4 '- (2 - ((2S) -1 - ((2S) -2 - ((METOXICARBONIL) AMINO) -3-METHYLBUTANOIL) -2-PIRROLIDINYL) -1H-IMIDAZOL-5-IL) -4-BIFENYLIL) -1H-IMIDAZOL-2-IL) - 1-PIRROLIDINIL

机译:合成((1S)-1-(((2S)二氯水合物盐((1S)-1-(((2S)-2-(5-(4'-(2-((2S)) -1-((2S)-2-((METOXICARBONIL)AMINO)-3-甲基丁二醇)-2-吡咯烷基)-1H-咪唑-5-IL)-4-苯乙腈)-1H-咪唑-2-IL)- 1-吡咯烷醇

摘要

1. This description generally relates to the synthesis of ((1s) - 1 - ((2S) - 2 - (5 - (4) - (2 - ((2S) - 1 - ((2S) - 1 - ((2S) - 2 - ((methylbonil) amino) - 3-methylbutane - (2-pirrolidinil) - 1 h-imidazol-5-il) - 4-bifenill -- 1 h-imidazol-2-il) - 1-pirr(olidinil) carbonil) - 2-methylpropylformate methyl ester. This disclosure also generally relates to intermediaries who are useful in this process. 1. Procedure for preparation of formula compound (7) or acceptable salts on its medicineWithin the EC, this is 0.1 or 2; s is 0, 1, 2, 3 or 4; u and V are selected from 0, 1, 2 or 3 respectively; X is selected from O, s, s (or).If n is 0, X is selected from CH2, CH5 and C (R5) 2; R1 and R2 are selected separately without considering Alcoy, hydrocarbon and halide; if s is 2, CH2, CH2, CH5 and C (R5) 2, each R5 is selected in the ring without considering alcox, hydrocarbon and arilo, Among them, tar can selectively form a concentration ring composed of 3-6 members with adjacent carbon atoms, and 3-6 members can optionally be replaced by one or two tar groups;The condition is that the two heterocycles replacing the imidazole ring are the same, including (a) reacting a formula compound (3), wherein u, V, R1 and R2 are as described in the formula (7);And...
机译:1.本说明通常涉及((1s)-1-((2S)-2-(5-(4)-(2-((2S)-1-((2S)-1-(( 2S)-2-((甲基甲基)氨基)-3-甲基丁烷-(2-吡咯烷基)-1 h-咪唑-5-il)-4-bifenill-1 h-咪唑-2-il)-1-pirr (奥地尼尔)羰基)-2-甲基丙基甲酸酯甲酯。该公开内容还通常涉及在该方法中有用的中间体1.制备通式化合物(7)或其药物可接受的盐的方法在EC内为0.1或2; s为0、1、2、3或4; u和V分别从0、1、2或3中选择; X从O,s,s(或)中选择;如果n为0,则选择X从CH2,CH5和C(R5)2中选择; R1和R2分别选择而不考虑醇,烃和卤化物;如果s为2,CH2,CH2,CH5和C(R5)2,则在环中选择每个R5考虑到醇,碳氢化合物和芳烃,其中的焦油可以选择性地形成由3-6个具有相邻碳原子的成员组成的浓环, ;和3-6个成员可以任选地被一个或两个焦油基团取代;条件是取代咪唑环的两个杂环是相同的,包括(a)使式化合物(3)反应,其中u,V,R 1和R 2如式(7)所述;并且...

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