55107-70-5

Usage

InChI:InChI=1/C4H8N2OS/c7-3-1-5-4(8)6-2-3/h3,7H,1-2H2,(H2,5,6,8)

Upstream product

• 75-15-0 carbon disulfide 
• 616-29-5 1,3-Diamino-2-hydroxypropane 

Downstream Products

• 669074-94-6 C₅H₁₀N₂OS 

Relevant academic research and scientific papers

Synthesis and DNA cleavage activity of 2-hydrazinyl-1,4,5,6-tetrahydropyrimidine containing hydroxy group

2-Hydrazinyl-1,4,5,6-tetrahydropyrimidin-5-ol dihydrochloride 2, as well as 2-hydrazinyl-4,5-dihydro-1H-imidazole dihydrochloride 1, was synthesized as metal-free DNA cleaving agent. Agarose gel electrophoresis was used to assess the plasmid pUC 19 DNA cleavage activities in the presence of 1 and 2. DNA cleavage efficiency of 2 exhibits remarkable increases compared with its corresponding non-hydroxy compound 1. Kinetic data of DNA cleavage promoted by 2 fit to the Michaelis-Menten-type equation with kmax of 0.0378 ± 0.0013 h-1 giving 106-fold rate acceleration over uncatalyzed DNA. The acceleration is driven by the spatial proximity of the nucleophilic hydroxy group and the electrophilic activation for the phosphodiester by the ammonium and/or guanidinium groups. In vitro cytotoxic activities toward Hela cells and human leukemia HL-60 cells were also examined, and 2 exhibits stronger cytotoxic activities than 1.

A Fast and Parallel Route to Cyclic Isothioureas and Guanidines with Use of Microwave-Assisted Chemistry

A fast and simple approach to novel cyclic isothioureas and related guanidine derivatives is presented in this study. The construction of the central basic scaffolds is achieved solely by the application of microwave-assisted chemistry, without any need of activating agents or protecting group manipulations. The product formation of various substituted guanidines from the corresponding isothiouronium salts was controlled by the nucleophilicity of the counterion and influenced by the reaction temperature. Further, a new fast-track access to tetrahydropyrimidin-2-ylamines was developed.

Pilot-plant preparation of an αvβ3 integrin antagonist. Part 2. Synthesis of N-[2-(5-hydroxy-4,6- tetrahydropyrimidine)]-3-amino-5-hydroxybenzoic acid

Studies directed toward the process research and development of a scalable method for preparing tetrahydropyrimidine 2, a key intermediate to the αvβ3 integrin antagonist 1, are described. A linear approach employing 3-amino-5-hydrox

PIPERIDINYL COMPOUNDS THAT SELECTIVELY BIND INTEGRINS

The invention is directed to piperidinyl compounds of formula (I) and (II) that selectively bind integrin receptors and methods for treating an integrin mediated disorder, wherein W, R2, Z and q are described in the application.

Condensed pyrrole mercapto compounds

The present invention relates to condensed pyrrole mercapto compounds, especially to optionally substituted indole or aza-indole mercapto derivatives, which compounds have ophthalmological and hypotensive properties, in particular vasoconstrictor, especially decongestant properties. It further relates to pharmaceutical compositions containing these compounds. An illustrative example is 3-(2-imidazolin-2-ylthio)-indole hydrochloride or hydroiodide.