公开(公告)号：EP1211239A1

公开(公告)日：2002-06-05

申请号：EP00956925.2

申请日：2000-09-05

申请人： Takeda Chemical Industries, Ltd.

发明人： IKEMOTO, Tomomi ,  ITO, Tatsuya, 117.1-7 Asahigaoka-Kukakuseirichinai ,  NISHIGUCHI, Atsuko ,  TOMIMATSU, Kiminori

IPC分类号： C07C229/18 ,  C07C227/14 ,  C07D223/16

CPC分类号： C07D223/16 ,  C07C229/18

摘要： As a process for preparing 2,3-dihydroazepine compounds at low cost in a simple and easy manner, there is provided a process for the preparation of compounds of the formula:
or salts thereof, characterized in that compounds of the formula:
or salts thereof are reacted with compounds of the formula:
or salts thereof to give compounds of the formula:
or salts thereof, which are then subjected to esterification and ring-closing reaction.

摘要翻译： 作为以简单和容易的方式低成本制备2,3-二氢氮杂化合物的方法，提供了制备下式化合物或其盐的方法，其特征在于下式化合物： 或其盐与下式化合物或其盐反应得到下式的化合物或其盐，然后进行酯化和闭环反应。

公开(公告)号：EP1445254A1

公开(公告)日：2004-08-11

申请号：EP02778097.2

申请日：2002-11-12

申请人： Takeda Chemical Industries, Ltd.

发明人： TAWADA, Hiroyuki ,  YAMASHITA, Makoto ,  IKEMOTO, Tomomi ,  NISHIGUCHI, Atsuko

IPC分类号： C07D231/20 ,  C07D417/12 ,  C07D413/12 ,  C07D401/12 ,  C07D413/14

CPC分类号： C07D401/12 ,  C07D231/20 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： As a method capable of conveniently producing a pyrazole compound in a high yield, which is useful as a synthetic intermediate for a pharmaceutical agent such as a therapeutic agent for diabetes and the like, a production method of a compound represented by the formula (I)
wherein n is an integer of 1 to 4 and R 1 is a hydrocarbon group optionally having substituents, or a salt thereof, is provided, which includes reacting a compound represented by the formula (II)
wherein Q is a hydroxy group optionally having substituents or an amino group optionally having substituents, R is a hydrocarbon group optionally having substituents and other symbols are as defined above, or a salt thereof, with hydrazine or a salt thereof.

摘要翻译： 作为能够以高收率制备吡唑化合物的方法，其可用作糖尿病治疗剂等药剂的合成中间体，由式（I）表示的化合物的制造方法， 其中n为1〜4的整数，R 1为任选具有取代基的烃基或其盐，其包括使式（II）表示的化合物反应其中Q 是任选具有取代基的羟基或任选具有取代基的氨基，R是任选具有取代基的烃基，其它符号如上所定义，或其盐与肼或其盐。

公开(公告)号：EP1334966A1

公开(公告)日：2003-08-13

申请号：EP01976719.3

申请日：2001-10-17

申请人： Takeda Chemical Industries, Ltd.

发明人： IKEMOTO, Tomomi ,  NISHIGUCHI, Atsuko ,  TOMIMATSU, Kiminori

IPC分类号： C07C311/51 ,  C07C311/14 ,  C07C311/28 ,  C07C303/40 ,  C07B57/00

CPC分类号： C07C311/51 ,  C07B2200/07 ,  C07C303/40 ,  C07C303/44 ,  C07C311/14 ,  C07C2601/16

摘要： A method including resolution of a diastereomeric mixture represented by the formula
wherein R 1 and R 2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, only one of R 1 and R 2 contains one asymmetric carbon, and R a is an optically active and optionally substituted hydrocarbon group or an optically active and optionally substituted heterocyclic group, or a salt thereof, to produce the diastereomer having a steric configuration of the asymmetric carbon for R 1 or R 2 of an R configuration or an S configuration, or a salt thereof.

摘要翻译： 由式 worin R表示的一个非对映体混合物的方法，包括分辨率<1>和R <2>是相同的或不同的，并各自为任选substituiertem烃基或在OPTIONALLY substituiertem杂环基团，只有R的一< 1>和R <2>含有一个不对称碳原子，和R a为光学活性和任选substituiertem烃基或以光学活性和任选substituiertem杂环基团，或它们的盐，以生产具有的立体构型非对映体 不对称碳为R构型的[R <1>或R <2>或S构型，或它们的盐。