147962-41-2

Usage

Uses

Used in Pharmaceutical Industry:
Propylsulfamide is used as an intermediate compound for the production of various medicines, including anti-convulsants and diuretics. Its unique composition allows it to play a vital role in the formulation of these drugs, contributing to their therapeutic effects.
Used in Antibacterial Applications:
Propylsulfamide is used as a key component in the production of sulfa drugs, which are commonly used to treat bacterial infections. Its presence in these drugs helps to combat bacterial pathogens, providing a valuable treatment option for various infections.

Upstream product

• 10305-42-7 N-propylsulfamoyl chloride 
• 107-10-8 propylamine 
• 1189-71-5 isocyanate de chlorosulfonyle 
• 1393813-40-5 tert-butyl (1-propyl)aminosulfonylcarbamate 

Downstream Products

• 1393813-42-7 N-5-(4-bromophenyl)-6-chloro-4-pyrimidinyl-N‘-propylsulfamide 

Relevant academic research and scientific papers

PYRIMIDINE SULFAMIDE DERIVATIVE AND PREPARATION METHOD AND MEDICAL APPLICATION THEREOF

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.

For horse west for tanzania intermediate preparation method (by machine translation)

The invention discloses a method for horse west for tanzania intermediate is third amidogen preparation of sulfonamides method, including: to propylamine and chloride as the starting material, triethylamine as acid-binding agent, through the two-step reaction is third amidogen sulfonamide crude product, after treatment distillation to obtain the states the propylamine base sulfonamide. Preparation method of this invention uses cheap and easily available raw materials, each step the reaction operation is simple, the reaction step and short reaction time, easy purification, high yield, low cost, and is suitable for industrial mass production. (by machine translation)

Synthesis and antitumor evaluation of novel sulfonylcycloureas derived from nitrogen mustard

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.

Simple, rapid, and clean condensation of sulfonamide and maleic anhydride derivatives: Synthesis of novel 1H- Pyrrole-2,5-diones under heterogeneous conditions

H6P2W18O62is used as an efficient catalyst for the synthesis of novel N-substituted sulfonyl maleimides (1H-Pyrrole-2,5-diones) via the condensation of sulfonamide and maleic anhydride derivatives. The Dawson heteropolyacid was used with a catalytic amount of 2?mmol% in acetonitrile at reflux. The reuse of H6P2W18O62as heterogeneous catalyst several times without decrease in their activity, short reaction times, easy isolation of desired products with good to excellent yields shows the advantages of this novel methodology.

PROCESS FOR PREPARING A PYRIMIDINE INTERMEDIATE

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.

Synthesis of new substituted N-sulfonyl pyrrolidine-2,5-dione using dawson-type heteropolyacid as catalyst

The synthesis of new series of pyrrolidine-2,5-diones having sulfonamide moieties is described. These compounds are synthesized in good yield in three steps (carbamoylation-sulfamoylation, deprotection and condensation) using a catalytic amount of H6P2W18O62 in acetonitrile under refluxing conditions.

PREPARATION OF PYRIMIDINE INTERMEDIATES USEFUL FOR THE MANUFACTURE OF MACITENTAN

The present invention relates to a new synthetic intermediate, namely the compound of formula I-2 I or a salt thereof. Said compound of formula I-2 or its salt can be used to prepare the compound of formula I-3 I which is an important synthetic intermediate used in the preparation of macitentan.

An efficient method for the synthesis of novel n-acylsulfonamides using tin (IV) chloride as catalysts

A series of novel N-acylsulfonamides derivatives were synthesized via direct condensation of parent sulfonamide with ethyl lactate as an acylating agent in the presence of tin (IV) chloride (SnCl4) as a Lewis acid catalyst. The sulfonamides were prepared, starting from chlorosulfonyl isocyanate (CSI), in three steps (carbamoylation, sulfamoylation, and deprotection) with excellent yields. Copyright

The discovery of N -[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy] ethoxy]-4-pyrimidinyl]- N ′-propylsulfamide (macitentan), an orally active, potent dual endothelin receptor antagonist

Starting from the structure of bosentan (1), we embarked on a medicinal chemistry program aiming at the identification of novel potent dual endothelin receptor antagonists with high oral efficacy. This led to the discovery of a novel series of alkyl sulfamide substituted pyrimidines. Among these, compound 17 (macitentan, ACT-064992) emerged as particularly interesting as it is a potent inhibitor of ETA with significant affinity for the ET B receptor and shows excellent pharmacokinetic properties and high in vivo efficacy in hypertensive Dahl salt-sensitive rats. Compound 17 successfully completed a long-term phase III clinical trial for pulmonary arterial hypertension.