4859-74-9

Upstream product

• 98-59-9 p-toluenesulfonyl chloride 
• 941-55-9 4-toluenesulfonyl azide 
• 949-01-9 1-(morpholin-4-yl)-2-phenylethanethione 
• 536-74-3 phenylacetylene 
• 110-91-8 morpholine 
• 884865-77-4 methyl N-(4-methylbenzenesulfonyl)phenylacetimidate 

Relevant academic research and scientific papers

Reactions of Thioacetamide Derivatives with Sulfonyl Azides: An Approach to Active-Methylene N-Sulfonylacetamidines

Reactions of functionalized [CN, CO2Et, C(O)NHR, C(S)NR1R2] derivatives of thiomalonic acid and 2-arylthioacetamides with sulfonyl azides were shown to give active-methylene N-sulfonylamidines in 62-98 yields. Various procedures for the reactions, including the use of pyridine, boiling ethanol, and water, or running the reactions in the absence of a base and solvent at 80 C, were carried out and compared. The solvent-free variant was the best in terms of yield, and also because it does not require the use of an excess of the toxic and hazardous azides. The reaction was shown to tolerate electron-withdrawing substituents such as carbonyl, cyano, and aryl groups at the C-2 position. The presence of alkyl and phenyl groups on the nitrogen atom of the thioacetamide fragment, and the presence of substituents on the sulfonyl group were also tolerated. Thus, an efficient solvent-free, catalyst-free, and base-free synthetic approach for the synthesis of N-sulfonylmalonacetamidines and 2-arylacetamidines was found. An efficient, solvent-free and base-free approach to active-methylene N-sulfonylacetamidines has been developed.

N-SULFONYL AMIDINE SYNTHESIS VIA THREE-COMPONENT COUPLING REACTION USING HETEROGENEOUS COPPER CATALYST

The present invention relates to a method of synthesizing N-sulfonyl amidine. More specifically, the present invention relates to the method of synthesizing N-sulfonyl amidine through a three-component coupling reaction using a heterogeneous copper catalyst; and optimization of reaction conditions applied thereto. The method is able to obtain corresponding N-sulfonyl amidine at high yield with respect to various substrates by performing a three-component coupling reaction of terminal alkyne, sulfonyl azide and amine by using a heterogeneous copper catalyst (Cu@C) obtained by pyrolyzing HKUST-1 which is a type of a metal-organic framework, and enables the heterogeneous copper catalyst to be reused at least four or more times without significant loss of catalytic activities since the heterogeneous copper catalyst has structural stability.COPYRIGHT KIPO 2018

N-Sulfonyl amidine synthesis via three-component coupling reaction using heterogeneous copper catalyst derived from metal-organic frameworks

Three-component coupling reaction of terminal alkyne, sulfonyl azide, and amine for the synthesis of N-sulfonyl amidine was developed using heterogeneous Cu@C catalyst, which was generated by pyrolysis of HKUST-1 (Cu3(BTC)2, BTC?=?1,

A facile access to N-sulfonylimidates and their synthetic utility for the transformation to amidines and amides

It is shown that N-sulfonylimidates can be efficiently prepared by a three-component coupling of terminal alkynes, sulfonyl azides, and alcohols with use of a copper catalyst and an amine base. The reaction is characterized by mild conditions, high select