公开(公告)号：EP2997031A1

公开(公告)日：2016-03-23

申请号：EP14732453.7

申请日：2014-05-16

申请人： Instytut Farmaceutyczny

发明人： MICHALAK, Olga ,  JATCZAK, Kamil ,  PUCKO, Wieslaw ,  WITKOWSKA, Anna ,  LASZCZ, Marta ,  BUJAK, Iwona ,  GROMAN, Aleksandra ,  CYBULSKI, Marcin

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： A process for the preparation of high purity amorphous pemetrexed disodium is characterized by reacting N-[4-[2-(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3- d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid with molar shortage of sodium cations generating compound in regard to carboxyl groups of free acid, under anhydrous conditions. Preferably, in that process pure crystalline Form 1 or Form 2 of N-[4-[2-(2- amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid, containing from 27 to 31% of dimethyl sulfoxide, is used.

公开(公告)号：EP2945961A1

公开(公告)日：2015-11-25

申请号：EP13828891.5

申请日：2013-12-30

申请人： Instytut Farmaceutyczny ,  Warszawski Uniwersytet Medyczny

发明人： GRUZA, Mariusz ,  JATCZAK, Kamil ,  LASZCZ, Marta ,  GRYNKIEWICZ, Grzegorz ,  GILLER, Tomasz ,  WITKOWSKA, Anna

IPC分类号： C07J63/00 ,  C07J71/00

CPC分类号： C07J63/008 ,  C07J71/0026

摘要： Process for preparation of 3,24;16,22-di-O,O-isopropylideneprotoescigenin comprises acetonidation of protoescigenin monohydrate in the mixture consisting of 0 - 100% vol. of acetone and 100 - 0% vol. of 2,2-dimethoxypropane, in presence of catalytic amount of an acid, furnishing precipitation of the crystalline product from the reaction mixture. 3,24; 16,22 -Di-O,O- isopropylideneprotoescigenin is isolated either in crystalline form A or B.

摘要翻译： 用于制备3,24; 16,22-二-O，O-异亚丙基原豆蔻醌的方法包括在由0-100％体积的组合物组成的混合物中对原水杨醇凝胶素一水合物进行乙酰化。 丙酮和100-0％体积。 的2,2-二甲氧基丙烷在催化量的酸存在下提供结晶产物从反应混合物中沉淀出来。 3,24; 以结晶形式A或B分离16,22-Di-O，O-异亚丙基原古菌素。