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1. CN102256984 - Method for producing diamine derivative

官庁 中華人民共和国
出願番号 200980151381.0
出願日 15.12.2009
公開番号 102256984
公開日 23.11.2011
特許番号 102256984
特許付与日 03.09.2014
公報種別 B
IPC
C07D 513/04
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
04オルソ―縮合系
A61K 31/444
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
4427さらに複素環系を含有するもの
444環異種原子として窒素を有する6員環を含むもの,例.アムリノン
A61P 7/02
A生活必需品
61医学または獣医学;衛生学
P化合物または医薬製剤の特殊な治療活性
7血液または細胞外液の疾患の治療薬
02抗トロンビン剤;抗凝血剤;血小板凝集阻害剤
CPC
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
A61P 7/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
A61P 7/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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
出願人 第一三共株式会社
発明者 小山威夫
優先権情報 2008-320693 17.12.2008 JP
発明の名称
(EN) Method for producing diamine derivative
(ZH) 制备二胺衍生物的方法
要約
(EN)
Provided is a method for producing a compound represented by formula (A) including: (a) a step of mixing a compound represented by formula (B) with p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate in an amount of less than one molar equivalent relative to the compound represented by formula (B) in a solvent while heating; (b) a step of adding p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate to the resulting mixed liquid while cooling, wherein the p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate to be added is added in an amount such that the total molar equivalent of the added p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate and the p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate in step (a) is one molar equivalent or more relative to the compound represented by formula (B); and (c) a step of obtaining a compound represented by formula (A) by crystallization.

(ZH)

本发明提供了制备式(A)所示的化合物的方法,该方法包括如下工序:(a)在加热下,将式(B)所示的化合物与相对于式(B)所示的化合物为小于1摩尔当量的对甲苯磺酸或对甲苯磺酸一水合物在溶剂中混合;(b)在冷却下,向所述混合溶液中加入额外的对甲苯磺酸或对甲苯磺酸一水合物,其中所述额外的对甲苯磺酸或对甲苯磺酸一水合物的加入量要使得其与工序(a)中的对甲苯磺酸或对甲苯磺酸一水合物的总摩尔当量相对于工序(a)中式(B)所示的化合物为1摩尔当量或更多;和(c)接着使所述混合溶液结晶以得到式(A)所示的化合物。

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