专利号:US-5998620-A 优先权日:1997-03-25 标 题 :Synthesis of intermediates useful in preparing tricyclic compounds 发明人:CHEN XING; POIRIER MARC; WONG YEE-SHING; WU GUANG-ZHONG 权利人:SCHERING CORP 摘要:The invention relates to a process for preparing a compound of the formula ##STR1## comprising reacting a bromo-substituted pyridine with an amine of the formula NHR 5 R 6 , reacting the resulting amide with an iodo-halomethyl-substituted compound and cyclizing the resultant product, wherein R, R 1 , R 2 , R 3 and R 4 are as defined in the specification; also claimed are a compound of the formula ##STR2## and a process for preparing it from the corresponding halo-substituted benzoic acid.
专利号:US-9243004-B2 优先权日:2011-07-22 标题 :Synthesis of boronic esters and boronic acids using grignard reagents 发明人:CLARY JACOB W; SINGARAM BAKTHAN 权利人:CLARY JACOB W; SINGARAM BAKTHAN; UNIV CALIFORNIA 摘要:Boronic esters and boronic acids are synthesized at ambient temperature in an ethereal solvent by the reaction of Grignard reagents with a boron-containing substrate. The boron-containing substrate may be a boronic ester such as pinacolborane, neopentylglycolborane, or a dialkylaminoborane compound such as diisopropylaminoborane. The Grignard reagents may be pre-formed or generated from an alkyl, alkenyl, aryl, arylalkyl, heteroaryl, vinyl, or allyl halide compound and Mg 0 . When the boron-containing substrate is a boronic ester, the reactions generally proceed at room temperature without added base in about 1 to 3 hours to form a boronic ester compound. When the boron-containing substrate is a dialkylaminoborane compound, the reactions generally proceed to completion at 0° C. in about 1 hour to form a boronic acid compound.
专利号:EP-0977739-B1 优先权日:1997-03-25 标题 :Synthesis of intermediates useful in preparing tricyclic compounds 发明人:CHEN XING; POIRIER MARC; WONG YEE-SHING; WU GUANG-ZHONG 权利人:SCHERING CORP 摘要:The invention relates to a process for preparing a compound of formula (I), comprising reacting a bromo-substituted pyridine with an amine of the formula NHR5R6, reacting the resulting amide with an iodo-halomethyl-substituted compound and cyclizing the resultant product, wherein R, R?1, R2, R3 and R4¿ are as defined in the specification; also claimed are a compound of formula (a), and a process for preparing it from the corresponding halo-substituted benzoic acid.
专利号:US-2014303333-A1 优先权日:2011-10-14 标题:Iron bisphenolate complexes and methods of use and synthesis thereof 发明人:SHAVER MICHAEL P; KOZAK CHRISTOPHER M 权利人:UNIV PRINCE EDWARD ISLAND; GENESIS GROUP INC 摘要:The present application, relates to iron bisphenolate complexes and methods of use and synthesis thereof. The iron complexes are prepared from tridentate or tetradentate ligands of Formula I: wherein R 1 and R 2 are as defined herein. Also provided are methods and processes of using the iron bisphenolate complexes as catalysts in cross-coupling reactions and in controlled radical polymerizations.
专利号:US-2022363662-A1 优先权日:2021-04-20 标题 :Compounds as lxr agonists 发明人:PUJALA BRAHMAM; SATHE BALAJI DASHRATH; DANODIA ABHINANDAN; GUPTA ASHU; SONI SANJEEV; KUMAR VIVEK; ANSARI AMANTULLAH; KHAN FARHA; SARKAR ARINDAM; PAYGHAN PAVAN V 权利人:INTEGRAL BIOSCIENCES PRIVATED LTD 摘要:The present invention generally discloses compounds having LXR (the liver X receptor) agonistic activity, to the use of such compounds in the treatment of various disorders such as proliferative disorders, Alzheimer's disease, inflammatory diseases, and diseases characterized by defects in cholesterol and lipid metabolism. Specifically, the present invention discloses compound of formula (IA) which exhibit LXR agonist activity, specifically to LXRβ. The invention also discloses method of synthesis of said compounds, method of using said compounds, pharmaceutical compositions comprising said compounds and method of using thereof.
专利号:US-2022411375-A1 优先权日:2019-10-18 标题:Process for synthesis of picolinamides
参考标题:Synthesis And Biological Activity Of Substituted 2,4-Diaminopyrimidines That Inhibit Bacillus Anthracis 作者:Baskar Nammalwar,Richard A. Bunce,K. Darrell Berlin,Christina R. Bourne,Philip C. Bourne,Esther W. Barrow,William W. Barrow |发布日期:2012.8 摘要:The Lowest Mics With Values Of 0.5 μg/ml And 0.375-1.5 μg/ml, Respectively. It Is Likely That The S Isomers Of 1 Will Bind The Substrate-Binding Pocket Of Dihydrofolate Reductase (Dhfr) As In B. Anthracis Was Found For (S)-1A. The Final Step In The Convergent Synthesis Of Target Systems 1 From (+/-)-1-(1-Substituted-2(1H)-Phthalazinyl)-2-Propen-1-Ones 6 With 2,4-Diamino-5-(5-Iodo-3,4-Dimethoxybenzyl)Pyrimidine
合成参考文献
摘要:Alonso, D. A.; Nájera, C., Science of Synthesis, (2010) 45, 243. 摘要:Gilchrist, T. L., Science of Synthesis, (2008) 43, 197. 摘要:Ohno, H.; Tomioka, K., Science of Synthesis, (2008) 44, 155. 摘要:Gagnon, A.; Benoit, E.; Le Roch, A., Science of Synthesis Knowledge Updates, (2018) 4, 2. 摘要:Song, Z.; Takahashi, T., Science of Synthesis Knowledge Updates, (2013) 1, 82.