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1. US20110275821 - Method for producing diamine derivative

官庁 アメリカ合衆国
出願番号 13162922
出願日 17.06.2011
公開番号 20110275821
公開日 10.11.2011
特許番号 08404847
特許付与日 26.03.2013
公報種別 B2
IPC
A61K 31/44
A生活必需品
61医学または獣医学;衛生学
K医薬用,歯科用又は化粧用製剤
31有機活性成分を含有する医薬品製剤
33複素環式化合物
395環異種原子として窒素を持つもの,例.グアネチジン,リファマイシン
435環異種原子として1個の窒素のみを有する6員環を持つもの,例.炭素環系と縮合したもの
44非縮合ピリジン;その水素添加誘導体
C07D 513/02
C化学;冶金
07有機化学
D複素環式化合物(高分子化合物C08)
513縮合系中に異項原子として窒素および硫黄原子のみをもつ少なくとも1個の複素環を含有し,C07D463/00,C07D477/00,またはC07D499/00~C07D507/00のグループに属さない複素環式化合物
02縮合系が2個の複素環を含有するもの
CPC
C07D 513/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
513Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/444
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
444containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
出願人 Koyama Takeo
Daiichi Sankyo Company, Limited
発明者 Koyama Takeo
代理人 Locke Lord LLP
優先権情報 2008-320693 17.12.2008 JP
発明の名称
(EN) Method for producing diamine derivative
要約
(EN)

The present invention provides a method for producing a compound represented by formula (A), the method comprising the steps of: (a) mixing a compound represented by formula (B) with p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate at less than 1 molar equivalent with respect to the compound represented by formula (B) in a solvent under heating; (b) adding additional p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate to the mixed solution under cooling, wherein the additional p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate is added in such an amount that the total molar equivalent thereof with the p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate of step (a) is 1 molar equivalent or more with respect to the compound represented by formula (B) of step (a); and (c) subsequently allowing the mixed solution to crystallize to obtain the compound represented by formula (A).