专利号:US-5783577-A 优先权日:1995-09-15 标题 :Synthesis of quinazolinone libraries and derivatives thereof 发明人:HOUGHTEN RICHARD A; OSTRESH JOHN M 权利人:TREGA BIOSCIENCES INC 摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.
专利号:US-6187923-B1 优先权日:1998-11-09 标题 :Process for the synthesis of quinazolinones 发明人:DENER JEFFREY MARK; LY CUONG QUOC 权利人:AXYS ADVANCED TECHNOLOGIES INC 摘要:The present invention provides a process for synthesizing a compound or a library of compounds of Formula 1A and 1B:
专利号:US-4308206-A 优先权日:1980-03-17 标 题:Process for preparing derivatives of 5,11-dihydro-6h-pyrido[2,3-b][1,4]-benzodiazepin-6-one, and the final derivatives and synthesis intermediates obtained thereby 发明人:GERSZBERG SZEPSEL 权利人:MICROSULES ARGENTINA SA 摘要:This invention relates to a process for preparing derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one of general formula (I) ##STR1## in which R is hydrogen, halogen or methyl; n R 1 and R 2 are linear or branched C 2 -C 4 alkyl groups, which alternatively may be joined together to give a piperazine cycle which can be substituted in position 4 with a methyl, ethyl or benzyl group, n and their salts with organic and inorganic acids, characterised by comprising the following stages: n (a) reacting a compound of general formula (X), ##STR2## in which R has the meaning heretofore defined, with 2-cloro-3-amino-pyridine of formula (III) ##STR3## in the presence of polyphosphoric acid, to give an intermediate of general formula (II) ##STR4## (b) reacting said intermediate with a compound of general formula (XI) ##STR5## in which R 1 and R 2 have the meaning heretofore defined and R 3 is a hydroxyl or halogen, in an inert solvent at a maximum temperature equal to the solvent boiling point, to give said derivatives of general formula (I). n The invention also relates to the final compounds thus obtained, and the synthesis intermediates obtained during the course of said process. n The final products of formula (I) are of great interest in the pharmaceutical field.
专利号:WO-0027831-A1 优先权日:1998-11-09 标题 :Process for the synthesis of quinazolinones
专利号:US-2011263569-A1 优先权日:2007-08-22 标 题 :Ryanodine channel binders and uses thereof 发明人:COREY ELIAS JAMES 权利人:HARVARD COLLEGE 摘要:Increasing the affinity of calstabin-2 for the cardiac calcium channel RyR2 and thereby stabilizing the channel in the closed state has recently been identified as novel mechanism for treating heart failure, particularly ventricular arrhythmias. JTV-519, a 1,4-benzothiazepine derivative, has been shown to stabilize the calstabin2/RyR2 complex. Novel derivatives of JTV-519 that may be useful in treatment or prevention of heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmias are provided. Synthetic methodology and intermediates in the synthesis of the inventive JTV-519 derivatives are also described.
专利号:WO-9811438-A1 优先权日:1996-09-13 标题 :Synthesis of quinazolinone libraries and derivatives thereof
[参考文献]: Joo Daniel Santos Fernandes, Et Al. The Role Of Amino Acid Permeases And Tryptophan Biosynthesis In Cryptococcus Neoformans Survival. Plos One. 2015 Jul 10;10(7):E0132369.
合成参考文献
摘要:Harris, P. A., Science of Synthesis Knowledge Updates, (2021) 3, 140. 摘要:Kang, F.-A.; Yang, S.-M., Science of Synthesis Knowledge Updates, (2015) 2, 190. 摘要:P. Leggate and G.E. Dunn. Can. J. Chem. 43, 1158 (1965). 摘要:P. Leggate and G. E. Dunn, Can. J. Chem. 43, 1158 (1965).