专利号:US-2013225819-A1 优先权日:2010-08-18 标 题:Use of azides in synthesis 发明人:JAMISON TIMOTHY F; PALDE PRAKASH B 权利人:JAMISON TIMOTHY F; PALDE PRAKASH B; MASSACHUSETTS INST TECHNOLOGY 摘要:Described herein are inventive methods for synthesis of tetrazoles. In some embodiments, the method involves the use of a flow reactor. The methods provided herein are capable at being carried out in short reaction times, with high yields, with minimal side reactions, and/or with minimal chance of explosions caused by the presence of azides.
专利号:US-6262272-B1 优先权日:1997-11-13 标题 :Method of synthesis of pyrrole amides 发明人:RAGAN JOHN ANTHONY; MAKOWSKI TERESA WOODALL; AM ENDE DAVID JON; CLIFFORD PAMELA JANE; YOUNG GREGORY RANDALL; CONRAD ALYSON KAY; EISENBEIS SHANE ALLEN; QUALLICH GEORGE JOSEPH; ALLEN DOUGLAS JOHN MELDRUM 权利人:PFIZER 摘要:A method for preparing pyrrole-carboxyamides which selectively bind to GABAa receptors; which comprises reacting 1,3-cycloakane-diones with bromoethylacetate followed by reaction of the resulting product with an acid halide followed by reaction with an aromatic amine and finally with an amonium source at an elevated temperature.
专利号:US-3919155-A 优先权日:1970-12-18 标题:Synthesis of aromatic amines by reaction of aromatic compounds with ammonia 发明人:SQUIRE EDWARD NOONAN 权利人:DU PONT 摘要:An improved process for producing an aromatic amine is provided in which an aromatic compound is reacted with ammonia in the presence of a conditioned nickel/nickel oxide cataloreactant at a temperature of from about 150*C. to about 500*C. and at a pressure of from about 10 to about 1000 atmospheres and in the presence of from 1 mole percent to 250 mole percent of water based on the molar amount of the aromatic compound.
专利号:US-4161609-A 优先权日:1977-09-14 标题:Synthesis of carboxylic acid esters 发明人:CRAMER RICHARD D 权利人:DU PONT 摘要:A method is provided for converting a carboxylic acid amide to a carboxylic acid ester by reacting a vaporized mixture of the amide and an aliphatic alcohol or a phenol in the presence of a suitable catalyst at temperatures of from 100 DEG C. to 400 DEG C. The process is especially useful for the conversion of methacrylamide to methyl methacrylate.
专利号:US-4031106-A 优先权日:1973-12-19 标题:Synthesis of aromatic amines by reaction of aromatic compounds with ammonia 发明人:DELPESCO THOMAS WAYNE 权利人:DU PONT 摘要:An improved process is provided for producing an aromatic amine from ammonia and an aromatic compound which comprises reacting the aromatic compound with ammonia at a temperature of from about 150 DEG C. to about 500 DEG C. and at a pressure of from about 10 to about 1000 atmospheres in the presence of a conditioned nickel/nickel oxide/zirconium oxide cataloreactant containing an oxide of lanthanum, samarium, holmium, europium, erbium, yttrium, praseodymium, neodymium, terbium, ytterbium, dysprosium or a mixture of any of them.
专利号:WO-2023245091-A1 优先权日:2022-06-15 标题 :Pyridazinone-derived compounds for the modulation of myc and for medical uses 发明人:ADANVE BERTRAND; NG YAO ZONG; LAI JONATHAN 权利人:GENETIC INTELLIGENCE INC 摘要:Compositions, systems, and methods are described herein for the modulation, and in particular the reduction or inhibition, of expression or activity of MYC in a cell, animal or human subject. Such compositions, systems, and methods are useful to prevent, ameliorate, or treat diseases, including cell proliferation diseases and disorders such as cancer, particularly MYC-driven cancer. Compositions are described comprising a compound of formula (I), as well as pharmaceutical compositions or medicaments thereof. Also described are methods of use of such compositions to treat, prevent, or ameliorate diseases, including cell proliferation diseases and disorders such as cancer, in particular MYC-driven cancer. Compositions comprising conjugates and complexes of a compound of formula (I) are also described, which are also useful in the methods described herein. Methods are described comprising the use of a compound of formula (I), or pharmaceutical compositions thereof, for the reduction or inhibition of MYC expression or activity, and/or for achieving one or more desirable phenotypic outcomes such as, for example, decrease in cancer cell growth or proliferation, decrease in cancer cell viability, decrease in tumor volume (i.e., tumor regression), decrease in cancer metastasis, increase in animal or human survival, or other desired outcome with respect to particular phenotypes (e.g., body weight, metabolism, etc.). Related medicaments, kits, and methods of delivery of such compositions are described. Methods are also described for the development, manufacture, and/or synthesis of a compound of formula (I), as well as pharmaceutical compositions thereof. Furthermore, methods for diagnostics and testing comprising detecting MYC expression or activity levels, as well as compositions comprising kits for diagnostics and testing, are described.