公开(公告)号：US20080125606A1

公开(公告)日：2008-05-29

申请号：US11656573

申请日：2007-01-23

申请人： Alain Burgos ,  Jacques Tonnel ,  Valerie Dambrin ,  Denis Lucet ,  Patricia Poirier

发明人： Alain Burgos ,  Jacques Tonnel ,  Valerie Dambrin ,  Denis Lucet ,  Patricia Poirier

IPC分类号： C07C213/02 ,  C07C47/04

CPC分类号： C07C213/02 ,  C07C2601/14 ,  C07C217/74

摘要： An in situ or one-pot process for the preparation of the compounds of formula (I) uses a compound of general formula (I): and includes:a) the hydrogenation of a nitrile group of the compound of general formula (II): in which R1 to R4 are especially H or alkyl and n varies from 0 to 4, in the presence of a hydrogenation catalyst, a methylating agent and an organic acid as solvent, and at a temperature Ta below the initiation temperature of a reductive amination reaction, to give a primary amine from the nitrile group; andb) the reductive amination of the primary amine in the presence of hydrogen, at a temperature Tb above Ta, to give the dimethylated amine of general formula (I) by activation of the methylating age.

摘要翻译： 用于制备式（I）化合物的原位或一锅法使用通式（I）的化合物：其包括：a）通式（II）的化合物的腈基的氢化： 其中R 1至R 4特别是H或烷基，n在0至4之间变化，在氢化催化剂，甲基化剂和作为溶剂的有机酸的存在下，在低于 还原胺化反应的起始温度，从腈基中得到伯胺; 和b）在氢存在下，在高于Ta的温度Tb下，伯胺的还原胺化，得到通过甲基化时代的活化的通式（I）的二甲基化胺。

公开(公告)号：US07462742B2

公开(公告)日：2008-12-09

申请号：US11656573

申请日：2007-01-23

申请人： Alain Burgos ,  Jacques Tonnel ,  Valéry Dambrin ,  Denis Lucet ,  Patricia Poirier

发明人： Alain Burgos ,  Jacques Tonnel ,  Valéry Dambrin ,  Denis Lucet ,  Patricia Poirier

IPC分类号： C07C209/00

CPC分类号： C07C213/02 ,  C07C2601/14 ,  C07C217/74

摘要： An in situ or one-pot process for the preparation of the compounds of formula (I) uses a compound of general formula (I): and includes:a) the hydrogenation of a nitrile group of the compound of general formula (II): in which R1 to R4 are especially H or alkyl and n varies from 0 to 4, in the presence of a hydrogenation catalyst, a methylating agent and an organic acid as solvent, and at a temperature Ta below the initiation temperature of a reductive amination reaction, to give a primary amine from the nitrile group; andb) the reductive amination of the primary amine in the presence of hydrogen, at a temperature Tb above Ta, to give the dimethylated amine of general formula (I) by activation of the methylating age.

摘要翻译： 用于制备式（I）化合物的原位或一锅法使用通式（I）的化合物：其包括：a）通式（II）的化合物的腈基的氢化： 其中R 1至R 4特别是H或烷基，n在0至4之间，在氢化催化剂，甲基化剂和作为溶剂的有机酸的存在下，并且在低于还原胺化反应的起始温度的温度Ta 从腈基中得到伯胺; 和b）在氢存在下，在高于Ta的温度Tb下，伯胺的还原胺化，得到通过甲基化时代的活化的通式（I）的二甲基化胺。