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カルベジロールの製造方法
专利权人:
シプラ・リミテッド
发明人:
ナラヤンラオ ラジェンドラ カンカン,ラマチャンドラ ドハルマラジ ラオ
申请号:
JP2007517424
公开号:
JP5118963B2
申请日:
2005.05.19
申请国别(地区):
JP
年份:
2013
代理人:
摘要:
The deviation from to benzyl converting benjirukarubejiroru which forms benjirukarubejiroru which is displayed with formula (vi) (vi), forms karubejiroru which is displayed with formula (i) (i) enantiomerism with pure form with respect to substance, or as the blend of enantiomer with in each case, depending upon when being the method of producing as those medical supplies as the salt which it can allow, 2,3- epokishipuropokishikarubazoru or the R or is displayed S enantiomer, with formula (v) (v) N- [the 2- (2- methoxy - phenoxy) ethyl] which are displayed with formula (ii) (ii) reacting with - benzyl amine, with catalytic hydrogenation, karubejiroru which is displayed with formula (i) the reflected imageOpposite sex with pure form with respect to substance, or as the blend of enantiomer it is the method if with in each case it forms, it is desire, this way where it is displayed with formula (i) reacting karubejiroru which was formed with inorganic or organic acid, of forming the salt which it can allow as that medical supply at the same time/or, it is desire, separating that enantiomer and. The aforementioned method the reaction with aforementioned 2,3- epokishipuropokishikarubazoru and the description above N- [the 2- (2- methoxy - phenoxy) ethyl] which is displayed with formula (v) - benzyl amine which is displayed with formula (ii), features that it executes at the underwater where it is reaction medium. In addition, this invention, offers karubejiroru, and the medicine composition which includes that and of using those for remedy the method of being displayed with formula (i) it manufactures with the kind of method the description above of doing.< Selective figure > Figure 1式(I)(I)で表されるカルベジロールを鏡像異性的に実質上純粋な形態で、又は鏡像異性体の混合物としてのいずれかで、場合によってはそれらの医薬品として許容し得る塩として製造する方法であって、式(II)(II)で表される2,3-エポキシプロポキシカルバゾール又はそのR若しくはS鏡像異性体を、式(V)(V)で表されるN-[2-(2-メトキシ-フェノキシ)エチル]-ベンジルアミンと反応させて、式(VI)(VI)で表されるベンジルカルベジロールを生成し、生成したベンジルカルベジロールを接触水素化によって脱ベンジル化して、式(I)で表されるカルベジロールを鏡像異性的に実質上純粋な形態で、又
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