- A PROCESS FOR PREPARATION OF TRIAMINOPYRIMIDINE COMPOUND AND INTERMEDIATES THEREOF
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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.
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Page/Page column 34
(2019/04/10)
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- Development of Scalable Processes for the Preparation of N-Methyl-3-Bromo-5-Methyl Pyrazole
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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.
- Fox, Richard J.,Markwalter, Chester E.,Lawler, Michael,Zhu, Keming,Albrecht, Jacob,Payack, Joseph,Eastgate, Martin D.
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p. 754 - 762
(2017/05/29)
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- Ni-Catalyzed C-H Functionalization in the Formation of a Complex Heterocycle: Synthesis of the Potent JAK2 Inhibitor BMS-911543
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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.
- 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.
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p. 6001 - 6011
(2015/06/30)
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- An Improved Synthesis of 3-(1-Imidazolyl)-2-alkenoic Acid Derivatives and Related Compounds
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The preparative method of 3-(1-imidazolyl)-2-alkenoic acid derivatives and the related compounds was improved by the use of strong bases such as sodium hydride in DMF.By this improved method, the preparation of 2-substituted 3-(1-imidazolyl)-2-alkenoic acid derivatives was accomplished in good yields.
- Kashima, Choji,Yoshiwara, Nobutoshi,Tajima, Tadakuni,Omote, Yoshimori
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p. 1595 - 1596
(2007/10/02)
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- The Compounds Related to 3-(1-Imidazolyl)-2-alken-1-ones. Preparation and Reactions
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Compounds related to 3-(1-imidazolyl)-2-alken-1-ones, 3-(1-imidazolyl)-2-alkenoic acid derivatives and 2-alken-1-ones having heterocycles on the C-3 carbon were prepared.The reaction of nucleophiles with these compounds was also discussed.
- Kashima, Choji,Tajima, Tadakuni,Omote, Yoshimori
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p. 171 - 176
(2007/10/02)
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- Immune-stimulating 1-(N-acylcarbamoyl)-2-cyanoaziridines
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1-(N-Acyl-carbamoyl)-2-cyanoaziridines of the formula STR1 wherein X is oxygen or sulphur, Z is hydrogen or an organic radical, and Y is a carbonyl, sulphonyl, sulphinyl, sulphenyl, phosphoryl or phosphonyl radical, and salts thereof, exhibit immune-stimulating and cancerostatic activities.
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