公开(公告)号：US20110263860A1

公开(公告)日：2011-10-27

申请号：US13125721

申请日：2009-10-23

Applicant: Yongjun Mao ,  Jianfeng Li ,  Jin Zheng ,  Zheng Liu ,  Kai Xie ,  Haihong Li ,  Jing Shi ,  Ye Li ,  Jingshan Shen

Inventor： Yongjun Mao ,  Jianfeng Li ,  Jin Zheng ,  Zheng Liu ,  Kai Xie ,  Haihong Li ,  Jing Shi ,  Ye Li ,  Jingshan Shen

IPC: C07D215/20 ,  C07D215/38 ,  C07C69/78

CPC classification number: C07C229/64 ,  C07C237/30 ,  C07C255/30 ,  C07D215/56

Abstract: The present invention relates to a method for preparing 6-substituted amino-3-cyanoquinoline compounds (compound A for short) and the intermediates thereof, more particularly, to a compound of the following formula (I), the preparation method thereof, the intermediates thereof and use thereof for preparing the compound A. The compound of the formula (I) is cyclized in the presence of an alkali to give a compound of formula A, wherein W is OH; or the compound of the formula (I) is cyclized in the presence of an alkali, and then chlorinated to give a compound of the formula A, wherein W is Cl. Compared with the known methods in the literature, the method for preparing the compound A from the compound of formula (I) according to the present invention can avoid using high-temperature condition and high boiling point solvents, and is safe and environment-friendly, mild in reaction condition, easy in operation with a high yield and high product purity.

Abstract translation: 本发明涉及一种制备6-取代氨基-3-氰基喹啉化合物（简称为化合物A）的方法及其中间体，更具体地涉及下式（I）的化合物，其制备方法，中间体 及其用于制备化合物A的用途。式（I）化合物在碱存在下环化，得到式A化合物，其中W为OH; 或式（I）化合物在碱的存在下环化，然后氯化，得到式A化合物，其中W为Cl。 与文献中已知的方法相比，本发明的式（I）化合物制备化合物A的方法可以避免使用高温条件和高沸点溶剂，且安全环保， 反应条件温和，易于操作，产率高，产品纯度高。

公开(公告)号：US08481741B2

公开(公告)日：2013-07-09

申请号：US13125721

申请日：2009-10-23

Applicant: Yongjun Mao ,  Jianfeng Li ,  Jin Zheng ,  Zheng Liu ,  Kai Xie ,  Haihong Li ,  Jing Shi ,  Ye Li ,  Jingshan Shen

Inventor： Yongjun Mao ,  Jianfeng Li ,  Jin Zheng ,  Zheng Liu ,  Kai Xie ,  Haihong Li ,  Jing Shi ,  Ye Li ,  Jingshan Shen

IPC: C07D215/38

CPC classification number: C07C229/64 ,  C07C237/30 ,  C07C255/30 ,  C07D215/56

Abstract: The present invention relates to a method for preparing 6-substituted amino-3-cyanoquinoline compounds (compound A for short) and the intermediates thereof, more particularly, to a compound of the following formula (I), the preparation method thereof, the intermediates thereof and use thereof for preparing the compound A. The compound of the formula (I) is cyclized in the presence of an alkali to give a compound of formula A, wherein W is OH; or the compound of the formula (I) is cyclized in the presence of an alkali, and then chlorinated to give a compound of the formula A, wherein W is Cl. Compared with the known methods in the literature, the method for preparing the compound A from the compound of formula (I) according to the present invention can avoid using high-temperature condition and high boiling point solvents, and is safe and environment-friendly, mild in reaction condition, easy in operation with a high yield and high product purity.

Abstract translation: 本发明涉及一种制备6-取代氨基-3-氰基喹啉化合物（简称为化合物A）的方法及其中间体，更具体地涉及下式（I）的化合物，其制备方法，中间体 及其用于制备化合物A的用途。式（I）化合物在碱存在下环化，得到式A化合物，其中W为OH; 或式（I）化合物在碱的存在下环化，然后氯化，得到式A化合物，其中W为Cl。 与文献中已知的方法相比，本发明的式（I）化合物制备化合物A的方法可以避免使用高温条件和高沸点溶剂，且安全环保， 反应条件温和，易于操作，产率高，产品纯度高。