64992-14-9Relevant articles and documents
Preparation method of theophylline sodium salt
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Paragraph 0041-0042; 0050-0052; 0058-0059; 0065-0066, (2020/09/08)
The invention relates to the technical field of pharmaceutical chemicals, and particularly discloses a preparation method of theophylline sodium salt. The preparation method of theophylline sodium salt comprises the following process steps: mixing cyanoacetic acid and acetic anhydride for reaction to obtain mixed anhydride, and performing a condensation reaction on the mixed anhydride and 1,3-dimethylurea to obtain 1,3-dimethyl cyanoacetylurea; sequentially carrying out cyclization, nitrosation, hydrogenation and acylation on the 1,3-dimethyl cyanoacetylurea to obtain 1,3-dimethyl-4-amino-5-formylamino uracil; subjecting the 1,3-dimethyl-4-amino-5-formylamino uracil to ring closing to obtain the theophylline sodium salt. According to the preparation method, the reaction conditions are mildand easy to control, the product yield is high, byproducts are few, strong ammonia gas smell is avoided, the cost is low, and generated pollution wastes are few.
Identification and Optimization of Novel Small c-Abl Kinase Activators Using Fragment and HTS Methodologies
Simpson, Graham L.,Bertrand, Sophie M.,Borthwick, Jennifer A.,Campobasso, Nino,Chabanet, Julien,Chen, Susan,Coggins, Julia,Cottom, Josh,Christensen, Siegfried B.,Dawson, Helen C.,Evans, Helen L.,Hobbs, Andrew N.,Hong, Xuan,Mangatt, Biju,Munoz-Muriedas, Jordi,Oliff, Allen,Qin, Donghui,Scott-Stevens, Paul,Ward, Paris,Washio, Yoshiaki,Yang, Jingsong,Young, Robert J.
supporting information, p. 2154 - 2171 (2019/02/26)
Abelson kinase (c-Abl) is a ubiquitously expressed, nonreceptor tyrosine kinase which plays a key role in cell differentiation and survival. It was hypothesized that transient activation of c-Abl kinase via displacement of the N-terminal autoinhibitory "myristoyl latch", may lead to an increased hematopoietic stem cell differentiation. This would increase the numbers of circulating neutrophils and so be an effective treatment for chemotherapy-induced neutropenia. This paper describes the discovery and optimization of a thiazole series of novel small molecule c-Abl activators, initially identified by a high throughput screening. Subsequently, a scaffold-hop, which exploited the improved physicochemical properties of a dihydropyrazole analogue, identified through fragment screening, delivered potent, soluble, cell-active c-Abl activators, which demonstrated the intracellular activation of c-Abl in vivo.
Studies on 3-oxoalkanenitriles: Novel rearrangement reactions observed in studies of the chemistry of 3-heteroaroyl-3-oxoalkanenitriles as novel routes to 2-dialkylaminopyridines
Al-Matar, Hamad M.,Khalil, Khaled D.,Al-Kanderi, Mona F.,Elnagdi, Mohamed H.
experimental part, p. 897 - 909 (2012/03/10)
3-Aroyl and 3-heteroaroyl substituted 3-oxoalkanenitriles were synthesized by the reactions of activated aromatic and hetero-aromatic substances with cyanoacetic acid in the presence of acetic anhydride. As part of studies focusing on the preparation of c
