Macitentan Impurity 26

Macitentan Impurity 26 - Names and Identifiers

Name	5-(4-Bromophenyl)-4,6-dichloropyrimidine
Synonyms	5-(4-broMophenyl)-4 Macitentan Impurity 26 Macitentan Intermediate 1 potassiuM (N-propylsulfaMoyl)aMide 5-(4-Bromophenyl)-4,6-dichloropyrimidine 5-(4-broMophenyl)-4,6-dichloropyriMidine 5-(4-Bromophenyl)-4,6-dichloro-Pyrimidin PyriMidine, 5-(4-broMophenyl)-4,6-dichloro- 5-(4-Bromophenyl)-4,6-dichloropyrimidine(146533-41-7)
CAS	146533-41-7

Macitentan Impurity 26 - Physico-chemical Properties

Molecular Formula	C10H5BrCl2N2
Molar Mass	303.97
Density	1.677±0.06 g/cm3(Predicted)
Melting Point	98.0 to 102.0 °C
Boling Point	368.7±42.0 °C(Predicted)
Solubility	Chloroform (Slightly), DMSO (Slightly)
Appearance	Solid
Color	Off-White
pKa	-4.92±0.26(Predicted)
Storage Condition	under inert gas (nitrogen or Argon) at 2-8°C
Use	Use 1. The intermediate of masitiptan is a reactant for the synthesis of mateptan, which is an orally active dual endothelin receptor antagonist. 2. The intermediate of masietiptan is mainly used as an intermediate for preparing masietiptan.

Macitentan Impurity 26 - Preparation method of 5-(4-bromophenyl)-4, 6-dichloropyrimidine

from Baidu library

Application (Patent) No.:

CN201810905221.1

date of application:

2018-08-09

public/announcement number:

CN108997223A

date of publication/announcement:

2018.12.14

Applicant (patentee):

Zhejiang Xianfeng Technology Co., Ltd

Inventor:

Gao Feifei ,< a href = "https://xueshu.baidu.com/s?wd=author: (Gao Junlong) & tn = SE_baiduxueshu_c1gjeupa & ie = utf-8 & SC _f_para = SC _hilight = person" target = "_blank"> Gao Junlong ,< a href = "https://xueshu.baidu.com/s?wd=author: (Zhu Minliang) & tn = SE_baiduxueshu_c1gjeupa & ie = utf-8 & SC _f_para = SC _hilight = person" target = "_blank"> Zhu Minliang , Lu Wei , Liu yi

national and provincial code:

CN331082

Summary:

The invention belongs to the technical field of pharmaceutical chemical synthesis, and relates to a preparation method of 5(4 bromophenyl) 4,6 dichloropyrimidine. The present invention includes the following steps, using p-bromophenylacetic acid catalytic esterification to produce p-bromophenylacetic acid methyl ester, and then react with dimethyl carbonate to synthesize 2(4 bromophenyl) malonic acid 1,3 diethyl ester, using formamidine hydrochloride to synthesize 5(4 bromophenyl) 4,6 dihydroxypyrimidine, and then chlorinated to obtain product 5(4 bromophenyl) 4,6. In the process of preparing intermediate 1, the present invention uses solid acid as a catalyst, which simplifies the synthesis process and post-treatment steps, and the solid acid is easy to separate, reusable, saves resources, and reduces production costs. In the process of preparing intermediate 2, sodium methoxide is used to replace sodium hydride or sodium amide used in the prior art as a base, which improves the safety of the reaction, reduces the cost of the reaction, and at the same time, the one-pot method is used to prepare intermediate 3, which reduces the operation steps.

Last Update：2024-01-02 23:10:35

Macitentan Impurity 26 - Reference Information

Use	Marcetane intermediate is a reactant used in the synthesis of mattetan, which is an orally active double endothelin receptor antagonist. marcetane intermediate
Overview	The trade name of macitentan is Opsumit. It is an oral ETA and ETB dual antagonist developed by the Swiss ActelionPharm. In October 2013, it was approved by FDA for the treatment of pulmonary hypertension, pulmonary fibrosis and other diseases. Since the product was launched, its effectiveness, safety and tolerance have performed well, and the market prospects are promising. 5-(4-bromophenyl)-4, 6-dichloropyrimidine is one of the intermediates of maxititan, which is mainly used to prepare maxititan.
Application	The intermediate of marcetane is mainly used as an intermediate for the preparation of marcetane.

Last Update：2024-04-09 21:04:16

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