52648-23-4

Upstream product

• 1072-98-6 5-chloro-2-pyridylamine 
• 6160-65-2 1,1'-Thiocarbonyldiimidazole 
• 463-71-8 thiophosgene 
• 88681-68-9 di(1H-imidazol-2-yl)methanethione 

Downstream Products

• 181305-44-2 1-(5-Chloro-pyridin-2-yl)-3-[2-(3-ethoxy-2-fluoro-6-methoxy-phenyl)-ethyl]-thiourea 
• 181305-49-7 1-(5-Chloro-pyridin-2-yl)-3-[2-(4-dimethylamino-2,6-difluoro-phenyl)-ethyl]-thiourea 
• 181305-42-0 1-(5-Chloro-pyridin-2-yl)-3-[2-(2-fluoro-3,6-dimethoxy-phenyl)-ethyl]-thiourea 
• 181305-21-5 1-(5-Chloro-pyridin-2-yl)-3-[2-(3-dimethylamino-2,6-difluoro-phenyl)-ethyl]-thiourea 

Relevant academic research and scientific papers

Synthesis and nematicidal activities of 1,2,3-benzotriazin-4-one derivatives containing thiourea and acylthiourea against Meloidogyne incognita

Two series of novel 1,2,3-benzotriazin-4-one derivatives containing thiourea and acylthiourea were designed and synthesized. The bioassay results showed that most of the test compounds showed good nematicidal activity against M. incognita at the concentration of 10.0?mg?L?1 in vivo. The compounds A13, A17 and B3 showed excellent nematicidal activity on the second stage juveniles of the root-knot nematode with the inhibition rate of 51.3%, 58.3% and 51.3% at the concentration of 1.0?mg?L?1 respectively. It suggested that the structure of 1,2,3-benzotriazin-4-one derivatives containing thiourea and acylthiourea could be optimized further.

Facile and versatile synthesis of alkyl and aryl isothiocyanates by using triphosgene and cosolvent

A mild and efficient method for the conversion of alkyl and aryl amines to isothiocyanates via dithiocarbamates has been developed using (CH 3)2CO-CS2 as co-solvent and triphosgene as dehydrosulfurization reagent. High yields, mild reaction conditions and excellent functional group compatibility make it become a versatile synthetic method for the preparation of isothiocyanates compared with reported methods. [Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications for the following free supplemental resource(s): Full experimental and spectral details.]

Catalytic enantioselective additions of indoles to nitroalkenes

A new design principle that provides access to more active thiourea catalysts is described. Highly enantioselective additions of indoles to nitroalkenes are reported using a new quinolinium thioamide catalyst. Copyright

Method for inhibition of HIV related viruses

Treatment of AIDS, inhibition of the replication of HIV and related viruses thereof, and formulations using thiourea derivative compounds or salts thereof is disclosed. Also disclosed are novel thiourea derivative compounds.

Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs

Phenylethylthiazolylthiourea (PETT) derivatives have been identified as a new series of nonnucleoside inhibitors of HIV-1 RT. Structure-activity relationship studies of this class of compounds resulted in the identification of N-[2-(2-pyridyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea hydrochloride (trovirdine; LY300046.HCl) as a highly potent anti-HIV-1 agent. Trovirdine is currently in phase one clinical trials for potential use in the treatment of AIDS. Extension of these structure-activity relationship studies to identify additional compounds in this series with improved properties is ongoing. A part of this work is described here. Replacement of the two aromatic moleties of the PETT compounds by various substituted or unsubstituted heteroaromatic rings was investigated. In addition, the effects of multiple substitution in the phenyl ring were also studied. The antiviral activities were determined on wild-type and constructed mutants of HIV-1 RT and on wild-type HIV-1 and mutant viruses derived thereof, Ile100 and Cys181, in cell culture assays. Some selected compounds were determined on double- mutant viruses, HIV-1 (Ile100/Asn103) and HIV-1 (Ile100/Cys181). A number of highly potent analogs were synthesized. These compounds displayed IC50's against wild-type RT between 0.6 and 5 nM. In cell culture, these agents inhibited wild-type HIV-1 with ED50's between I and 5 nM in MT-4 cells. In addition, these derivatives inhibited mutant HIV-1 RT (Ile 100) with IC50's between 20 and 50 nM and mutant HIV-1 RT (Cys 181) with IC50's between 4 and 10 nM, and in cell culture they inhibited mutant HIV-1 (Ile100) with ED50's between 9 and 100 nM and mutant HIV-1 (Cys181) with ED50's between 3 and 20 nM.

Substituted pyrido-triazines as anthelmintics

Pyrido-(1,2-a)-1,3,5-triazines which are variously substituted on the triazine ring at the 3-position and on the pyridine ring on any of the available positions are active anthelmintic and antifungal agents and are prepared by condensing a substituted isocyanate or an isothiocyanate with a pyridyl-isocyanate or isothiocyanate. The compounds are disclosed in compositions and methods for the treatment of helminthiasis and fungal diseases.