147962-41-2Relevant articles and documents
PYRIMIDINE SULFAMIDE DERIVATIVE AND PREPARATION METHOD AND MEDICAL APPLICATION THEREOF
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Paragraph 0102; 0105-0106, (2020/09/22)
Disclosed are a series of pyrimidine sulfamide compounds and applications thereof in preparing a drug for a disease related to an ETA receptor antagonist. In particular, disclosed is a derived compound represented by formula (I) or a tautomer or pharmaceutically acceptable composition thereof.
Synthesis and antitumor evaluation of novel sulfonylcycloureas derived from nitrogen mustard
Cheloufi,Belhani,Ouk,Zerrouki,Aouf,Berredjem
, p. 399 - 405 (2016/04/20)
A new series of sulfonylcycloureas derivatives have been synthesized and evaluated in vitro for their antitumor activity against four cancer cell lines (A431, Jurkat, U266, and K562). These compounds were prepared by the condensation of several sulfonamides (2am) with ethyl bis(2-chloroethyl)carbamate (1a). The relative cytotoxicity of these new derivatives in comparison to chlorambucil is reported.
PROCESS FOR PREPARING A PYRIMIDINE INTERMEDIATE
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Page/Page column 25; 26, (2015/02/02)
The present invention relates to a process for preparing a pyrimidine intermediate, namely the compound of formula I-2 or a salt thereof. Said compound of formula I-2 or its salt can be used to prepare macitentan. Macitentan (chemical names: N-[5-(4-bromophenyl)-6-[2-[(5-bromo- 2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl] -N'-propylsulfamide or N-[5-(4-bromophenyl)- 6- {2- [(5 -bromopyrimidin-2-yl)oxy] ethoxy } pyrimidin-4-yl] -N'-propylsulfuric diamide) is an endothelin receptor antagonist that has notably been approved by the US Food and Drug Administration and the European Commission for the treatment of pulmonary arterial hypertension. It has been first disclosed in WO 02/053557. The last step of one of the potential preparation routes described in WO 02/053557, called Possibility A and Possibility B , can be summarised as shown in Scheme Al hereafter.