29594-65-8

Upstream product

• 447-31-4 Desyl chloride 
• 103-85-5 monophenylthiourea 
• 72149-84-9 1-[1-Methoxy-1-phenyl-meth-(Z)-ylidene]-3-phenyl-thiourea 
• 333-20-0 potassium thioacyanate 
• 62-53-3 aniline 
• 1484-50-0 desyl bromide 
• 451-40-1 phenyl benzyl ketone 
• 72149-84-9 1-(methoxyphenylmethylene)-3-phenylthiourea 
• 100-39-0 benzyl bromide 
• 100-16-3 4-nitrophenylhydrazone 
• 199915-38-3 9-fluorenylmethoxycarbonyl isothiocyanate 

Relevant academic research and scientific papers

Reaction of mercaptoacetate and halides containing activated methylenes with thiocarbamoylimidates: A novel approach to the synthesis of aminothiazole derivatives

The reaction of N-thiocarbamoylimidates 1 with methyl thioglycolate leads to the formation of 4-arylamino-5-methoxycarbonylthiazoles 2. The condensation of the same imidates 1 on ethyl bromoacetate, benzyl bromide and chloroacetonitrile provides the corre

Traceless solid-phase synthesis of 2-aminothiazoles: Receptor tyrosine kinase inhibitors with dual selectivity for tie-2 and VEGFR-2

A 10-step (!) solid-phase synthesis employing the traceless hydrazide linker provides efficient access to a 2-aminothiazole library (see scheme) that yielded access to a new class of tyrosine kinase inhibitors with dual selectivity for the vascular endothelial growth factor receptor VEGFR-2 and the Tie-2 receptor tyrosine kinases.

Reaction of mercaptoacetate and halides containing activated methylenes with thiocarbamoylimidates: A novel approach to the synthesis of aminothiazole derivatives

The reaction of N-thiocarbamoylimidates 1 with methyl thioglycolate leads to the formation of 4-arylamino-5-methoxycarbonylthiazoles 2. The condensation of the same imidates 1 on ethyl bromoacetate, benzyl bromide and chloroacetonitrile provides the corre

Synthesis of 5-Phenylthiazolamines by Using Thiourea as an α-Bromination Shuttle

A straightforward synthesis of 5-phenylthiazolamines by coupling thiourea with phenylacetones, phenylacetophenones, and β-tetralone has been developed. Thiourea acts as a substrate and an α-bromination shuttle by transferring a Br atom from CBrCl3/s

Cyclocondensations of substituted thiosemicarbazides with 2-bromo-1,2-diphenylethan-1-one

The cyclocondensation of 4-methylthiosemicarbazide with 2-bromo-1,2-diphenylethan-1-one in ethanol afforded isomeric 2-methylamino-5,6-diphenyl-6H-3,4-thiadiazine and 2-hydrazono-3- methyl-4,5-diphenyl-2,3-dihydro-1,3-thiazole. A pyrazole was obtained by cyclocondensation and subsequent desulfurization of the thiadiazine when the reaction was carried out in concentrated hydrochloric acid. A chemical proof of the structures has been provided. The product distribution of the cyclizations strongly depends on the substitution pattern of the starting materials, and the cyclizations of methylthiosemicarbazide with 2-bromo-1,2-diphenylethan-1-one behaved considerably different from that of the analogous reactions of α-bromoacetophenone.

Microwave promoted synthesis of functionalized 2-aminothiazoles

Microwave irradiation promotes the rapid one-pot synthesis of 2-aminothiazoles fromed via the condensation of α-bromoketones with thiourea.

Multistep solid-phase synthesis of an antibiotic and receptor tyrosine kinase inhibitors using the traceless phenylhydrazide linker

The hydrazide group is an oxidatively cleavable traceless linker for solid-phase chemistry. This linker technology was used to develop a multistep solid-phase synthesis of an antibiotic that is active against Mycobacterium tuberculosis. Furthermore, we describe an efficient method for the traceless synthesis of 2-aminothiazoles that display dual inhibitory activity against the receptor tyrosine kinases VEGFR-2 and Tie-2. The synthesis method proceeds through 9 steps on the solid phase and should give access to a much larger library of 2-aminothiazoles, from which a new class of anti-angiogenesis drugs may be developed.

One-pot synthesis of 2-aminothiazoles using supported reagents

A simple and efficient method has been developed for the synthesis of 2-aminothiazoles from α-bromo ketones in one-pot using a supported reagents system, KSCN/SiO2-RNH3OAc/Al2O3, in which α-bromo ketone reacts first with KSCN/SiO2 and the product, α-thiocyano ketone, reacts with RNH3OAc/Al2O3 to give the final product, 2-aminothiazole, in high yield.