35100-92-6Relevant academic research and scientific papers
A PROCESS FOR PREPARATION OF TRIAMINOPYRIMIDINE COMPOUND AND INTERMEDIATES THEREOF
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Page/Page column 34, (2019/04/10)
The present invention relates to triaminopyrimidine compound 1, or pharmaceutically acceptable salts thereof, or hydrates, or solvates, or polymorphs, or optically active forms thereof, in solid state forms. The invention also relates to a process for preparation of triaminopyrimidine compound and intermediates thereof. The present invention also relates to a pharmaceutical composition comprising pure triaminopyrimidine compound, useful for preventing or treating malaria.
Development of Scalable Processes for the Preparation of N-Methyl-3-Bromo-5-Methyl Pyrazole
Fox, Richard J.,Markwalter, Chester E.,Lawler, Michael,Zhu, Keming,Albrecht, Jacob,Payack, Joseph,Eastgate, Martin D.
, p. 754 - 762 (2017/05/29)
The development and optimization of two scalable routes to N-methyl-3-bromo-5-methyl pyrazole is described. The initial Sandmeyer route entailed a three-step sequence from crotonitrile and methyl hydrazine, proceeding through the 3-amino pyrazole intermediate. Due to the GTI liability of the 3-amino pyrazole intermediate, a tedious steam-distillation, and 30% overall yield, we developed a second-generation Sandmeyer-free approach from methyl crotonate and methyl hydrazine which leveraged a condensation, bromination, and oxidation sequence. Process development led to the improved preparation of N-methyl-3-bromo-5-methyl pyrazole with increased efficiency and overall yield. The isolation, handling, and storage of the final product was greatly improved through the generation of the triflic acid salt, and salt form studies are also discussed.
SULFONYLUREAS AND RELATED COMPOUNDS AND USE OF SAME
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Page/Page column 139, (2016/09/15)
ABSTRACT The present invention provides for certain sulfonyl ureas and related compounds which have advantageous properties and show useful activity in the inhibition of activation of the NLRP3 inflammasome. Such compounds are useful in the treatment of a wide range of disorders in which the inflammation process, or more specifically the NLRP3 inflammasome, have been implicated as being a key factor.
Ni-Catalyzed C-H Functionalization in the Formation of a Complex Heterocycle: Synthesis of the Potent JAK2 Inhibitor BMS-911543
Fitzgerald, Monica A,Soltani, Omid,Wei, Carolyn,Skliar, Dimitri,Zheng, Bin,Li, Jun,Albrecht, Jacob,Schmidt, Michael,Mahoney, Michelle,Fox, Richard J.,Tran, Kristy,Zhu, Keming,Eastgate, Martin D.
, p. 6001 - 6011 (2015/06/30)
BMS-911543 is a complex pyrrolopyridine investigated as a potential treatment for myeloproliferative disorders. The development of a short and efficient synthesis of this molecule is described. During the course of our studies, a Ni-mediated C-N bond formation was invented, which enabled the rapid construction of the highly substituted 2-aminopyridine core. The synthesis of this complex, nitrogen-rich heterocycle was accomplished in only eight steps starting from readily available materials.
HETROARYL BENZAMIDE DERIVATIVES FOR USE AS GLK ACTIVATORS IN THE TREATMENT OF DIABETES
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Page/Page column 187, (2008/06/13)
Compounds of Formula (I) wherein: R1 is hydroxymethyl; R2 is selected from -C(O)NR4R5, SO2NR4R5, S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.
Aminopyrazoles. IV. Pyrazol-3- and 5-amines from 2,3-dihaloalkanenitriles or 3-Chloroacrylonitriles and Hydrazines
Ege, Guenter,Franz, Hermann
, p. 1267 - 1273 (2007/10/02)
2,3-Dihalopropanenitriles and substituted 3-chloropropenenitriles react with hydrazines in basic solution to form either pyrazol-3-amines 4 or pyrazol-5-amines 5 or a mixture of both isomers.
