180791-02-0

Upstream product

• 33252-30-1 2-chloro-4-pyridinenitrile 
• 100-53-8 phenylmethanethiol 
• 100-44-7 benzyl chloride 
• 100-51-6 benzyl alcohol 

Downstream Products

• 100727-33-1 2-benzylmercapto-isonicotinic acid 

Relevant academic research and scientific papers

Synthesis of 2-benzylthiopyridine-4-carbothioamide derivatives and their antimycobacterial, antifungal and photosynthesis-inhibiting activity

A series of 2-benzylthiopyridine-4-carbonitriles 4 and a series of 2- benzylthiopyridine-4-carbothioamides 5 were prepared. Their chemical structures were proved by IR and 1H NMR data and by elemental analysis. The MIC assessment was used for the estimation of their potential antimycobacterial and antifungal activity in vitro. The compounds were shown to be more active against mycobacterial strains than the tested fungi. Their antimycobacterial activity appears to be related mainly to the benzylthio moiety, while the antifungal activity appears to be related to the carbothioamide group. Substituents on the benzylthio moiety of derivatives 5 modified antifungal activity, whereas they did not play any significant role in antimycobacterial activity. The inhibiting effect of 4 and 5 on the photochemical activity of spinach chloroplasts was determined by IC50 values. The compounds exhibited a moderate photosynthesis-inhibiting activity.

SUBSTITUTED SULFONAMIDE PYRROLOPYRIDINES AS JAK INHIBITORS

The present invention relates to new sulfonamide pyrrolopyridine compounds and compositions useful in the treatment of JAK-mediated conditions having the structures of Formula (I), wherein the R groups are as defined in the detailed description. Methods o

Promoting Effect of Crystal Water Leading to Catalyst-Free Synthesis of Heteroaryl Thioether from Heteroaryl Chloride, Sodium Thiosulfate Pentahydrate, and Alcohol

It is observed the crystal water in sodium thiosulfate pentahydrate (Na2S2O3·5H2O) can promote its multicomponent reaction with heteroaryl chlorides and alcohols, providing a facile, green, and specific synthesis of unsymmetrical heteroaryl thioethers via one-step formation of two C-S bonds under catalyst-, additive-, and solvent-free conditions. Mechanistic studies suggest that the crystal water in Na2S2O3·5H2O is crucial in generating the key thiol intermediates and byproduct NaHSO4, which then catalyzes the dehydrative substitution of alcohols with thiols to afford thioethers.

Efficient Generation of C–S Bonds via a By-Product-Promoted Selective Coupling of Alcohols, Organic Halides, and Thiourea

A metal- and base-free three-component coupling of alcohols, heteroaryl halides, and thiourea has been developed for direct and selective synthesis of heteroaryl thioethers. This method can be easily scaled up to the gram scale and extended to dialkyl thioethers, heteroaryl selenides, benzothiazoles, and some antimycobacterially-active thioethers. Mechanistic studies revealed that a by-product-promoted in situ C–O activation of alcohols to more reactive alkyl halides and slow release of the thiol and alkyl halide intermediates are the key to the high selectivity and success of the reaction. (Figure presented.).

PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES USEFUL FOR INHIBITING JANUS KINASE

Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing them, and therapeutic uses thereof.

PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES

Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.

Some anilides of 2-alkylthio- and 2-chloro-6-alkylthio-4-pyridinecarboxylic acids: Synthesis and photosynthesis-inhibiting activity

Many compounds containing a -CONH- group display photosynthesis inhibiting activity. Based on this structural feature, a group of anilides of 2-alkylthio-(1b-4f) or 2-chloro-6-alkylthio-4-pyridinecarboxylic acids (5a-6c) was synthesised. The prepared compounds were tested for their inhibition of the oxygen evolution rate (OER) in spinach chloroplasts. A quasi-parabolic dependence between photosynthesis-inhibiting activity and the lipophilicity of the compounds was determined for 1b-4f as well as for 5a-6c. The inhibitory activity of compounds 1b-4f was higher than that of 5a-6c for comparable lipophilicity values.

Potential antifungal agents. Synthesis and activity of 2-alkylthiopyridine-4-carbothioamides

A series of 2-alkylthiopyridine-4-carbothioamides were synthesized, and their antifungal potency was tested. The chemical structures were proved by IR and 1H-NMR data and by elemental analysis. The MIC and MFC assessment were used for the estimation of potential activity in vitro. The study comprising 21 clinical isolates of fungi showed that compounds 5h and 5j exhibited fair inhibitory activity against some yeasts and dermatophytes. Selective fungistatic activity against dermatophytes (MIC = 3.12-25.0 μg/mL) was found also in compound 5g. None of the above compounds showed inhibitory activity against non-dermatophyte filamentous fungi. Microbiological activity of 2-alkylthiopyridine-4-carbothioamides appears to be mainly related to hydrophobicity of alkyl in position 2.