Category: 2136287-65-3

Zhou, Zihong published the artcileDevelopment of a Quality Controllable and Scalable Process for the Preparation of 7,8-Difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-ol: A Key Intermediate for Baloxavir Marboxil, Category: catalysis-chemistry, the publication is Organic Process Research & Development (2019), 23(12), 2716-2723, database is CAplus.

A novel six-step synthesis of 7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-ol is described. Starting with 3,4-difloro-2-methylbenzoic acid and using di-Ph disulfide as an ideal sulfur source effectively solve the problems such as harsh reaction conditions, usage of smelly thiophenol, which might restrict the known process from pilot plant application. Large-scale applicability of this new route has been successfully demonstrated on kilogram-scale production to afford 7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-ol with 98.04% purity in 75% overall yield. Meanwhile, the corresponding impurity profile was thus studied in detail and well documented.

Organic Process Research & Development published new progress about 2136287-65-3. 2136287-65-3 belongs to catalysis-chemistry, auxiliary class Fluoride,sulfides,Carboxylic acid,Benzene, name is 3,4-Difluoro-2-((phenylthio)methyl)benzoic acid, and the molecular formula is C19H14N2, Category: catalysis-chemistry.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Taoda, Yoshiyuki published the artcileDihydrodibenzothiepine: Promising hydrophobic pharmacophore in the influenza cap-dependent endonuclease inhibitor, Application In Synthesis of 2136287-65-3, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(22), 127547, database is CAplus and MEDLINE.

This work describes a set of discovery research studies of an influenza cap-dependent endonuclease (CEN) inhibitors with a carbamoyl pyridone bicycle (CAB) scaffold, particularly dibenzothiepine-substituted pyridotriazinediones such as I. Using influenza CEN inhibitory activity, antiviral activity and pharmacokinetic (PK) parameters as indexes, structure activity relationships (SAR) studies were performed at the N-1 and N-3 positions on the CAB scaffold, which is a unique template to bind two metals. The hydrophobic substituent at the N-1 position is extremely important for CEN inhibitory activity and antiviral activity, and dihydrodibenzothiepine was the most promising pharmacophore. I showed potent virus titer reduction over oseltamivir phosphate in an in vivo mouse model. I served as the lead compound of baloxavir marboxil with a tricyclic scaffold, which was approved in Japan and the USA in 2018.

Bioorganic & Medicinal Chemistry Letters published new progress about 2136287-65-3. 2136287-65-3 belongs to catalysis-chemistry, auxiliary class Fluoride,sulfides,Carboxylic acid,Benzene, name is 3,4-Difluoro-2-((phenylthio)methyl)benzoic acid, and the molecular formula is C9H7NO4, Application In Synthesis of 2136287-65-3.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia