On December 31, 2014, Ko, Soo Sung; Batt, Douglas A.; Bertrand, Myra Beaudoin; Delucca, George V.; Langevine, Charles M.; Liu, Qingjie; Srivastava, Anurag S.; Watterson, Scott Hunter published a patent.Recommanded Product: 1-Bromo-3-isocyanato-2-methyl-benzene The title of the patent was Preparation of 4-phenylcarbazole-1-carboxamide compounds useful as Bruton’s tyrosine kinase (Btk) inhibitors. And the patent contained the following:
There are disclosed carbazolecarboxamide compounds of formula [I; Q = Q1, Q2, Q3, or Q4; R1 = C(CH3)2OH, NHC(O)C(CH3)3, N(CH3)2, or CH2Rd; R2 = Cl or CH3; R3 = H, F, or CH3; Ra = H or CH3; Rb = H, F, Cl, or OCH3; Rc = H or F; Rd = OH, OCH3, NHC(O)CH3, or pyrrolidin-1-yl] or salts thereof. These compounds are inhibitors of kinases, in particular Bruton’s tyrosine kinase (Btk) and are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and chronic inflammatory diseases. Thus, 4-bromo-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide was coupled with 5-chloro-2-[2-methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]-1H-pyrido[1,2-c]pyrimidine-1,3(2H)-dione in the presence of Pd2(dppf).CH2Cl2adduct and Cs2CO3 in THF under argon at 45° for 3.5 h to give 39% 4-[3-(5-chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrimidin-2(3H)-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide as a mixture of 4 diastereomers which was separated by chiral super-critical fluid chromatog. to give 4-[3-(R)-(5-Chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrimidin-2(3H)-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide (II) and 4-[3-(S)-(5-chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrimidin-2(3H)-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide (III). III showed IC50 of 0.41 and 1,000 nM against human recombinant Bruton’s tyrosine kinase (Btk) and Jak2 tyrosine kinase, resp. The experimental process involved the reaction of 1-Bromo-3-isocyanato-2-methyl-benzene(cas: 1261475-16-4).Recommanded Product: 1-Bromo-3-isocyanato-2-methyl-benzene
The Article related to carbazolecarboxamide preparation bruton tyrosine kinase btk kinase inhibitor, phenylcarbazolecarboxamide preparation kinase inhibitor, autoimmune disease chronic inflammatory disease treatment prevention phenylcarbazolecarboxamide preparation and other aspects.Recommanded Product: 1-Bromo-3-isocyanato-2-methyl-benzene
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