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Dibenzo [b, d] the production method of azepin-6-one derivatives
专利权人:
エフ.ホフマン-ラ;アーゲー;ロシュ;エフ.ホフマン-ラ ロシュ アーゲー
发明人:
ホフマン-エメリー,ファビエンネ,ヤコブ-レートネ,ローラント,ホフマン-エメリー,ファビエンネ,ヤコブ-レートネ,ローラント
申请号:
JP2010508802
公开号:
JP5745841B2
申请日:
2008.05.15
申请国别(地区):
JP
年份:
2015
代理人:
摘要:
The invention relates to a process for the optical resolution of a dibenzo[b,d]azepinone derivative of formula II, wherein R1 is hydrogen or halogen and R2 is either C1-4-alkyl optionally substituted with C3-7-cycloalkyl or benzyl which is optionally substituted with C1-4-alkoxy, to obtain a (S)-7-amino-5H,7H-dibenzo[b,d]azepin-6-one of formula I, wherein R1 is as in the compound of formula II. The (S)-7-amino-5H,7H-dibenzo[b,d]azepin-6-one of formula I can be used as a chiral building block for the preparation of malonamide derivatives which have the potential to act as gamma-secretase inhibitors and therefore may be useful in the treatment of Alzheimer's disease and cancer.
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