5-溴-6-甲基-2-甲硫基-1H-嘧啶-4-酮置于硫酸,氨,锌,三氯氧磷,苯体系中,化学反应生成 2,4-二氯-6-甲基嘧啶 参考文献:Matsukawa; Ohta,Yakugaku Zasshi/journal Of The Pharmaceutical Society Of Japan,1950,Vol. 70,P. 137 标题:Matsukawa; Ohta,Yakugaku Zasshi/journal Of The Pharmaceutical Society Of Japan,1950,Vol. 70,P. 137
专利信息
专利号:US-7576245-B2 优先权日:2002-07-11 标题:Fluorous tagging and scavenging reactants and methods of synthesis and use thereof 发明人:ZHANG WEI; LUO ZHIYONG 权利人:FLUOROUS TECHNOLOGIES INC 摘要:The present invention includes methods and compositions for increasing the fluorous nature of an organic compound by reacting it with at least one fluorous compound to produce a fluorous tagged organic compound. The increased fluorous nature of the fluorous tagged organic compound can then be utilized to separate the fluorous organic compound from untagged reagents, reactants, catalysts and/or products derived therefrom. The resultant fluorous tagged organic compound can be subjected to subsequent chemical transformations, wherein the fluorous nature of the tagged compound is utilized to increase the ease of separation of the fluorous tagged organic compound from untagged reagents, reactants, catalysts and/or products derived therefrom, after each chemical transformation. The chemical transformations result in a second fluorous tagged organic compound wherein the fluorous nature of the second fluorous tagged organic compound can then be reduced by removing the fluorous group therefrom, thereby producing a second organic compound that may be employed as a pharmaceutical compound or intermediate, or a combinatorial library component.
专利号:US-6552018-B1 优先权日:1997-01-27 标 题:Pyrazole derivatives 发明人:EJIMA AKIO; OHSUKI SATORU; OHKI HITOSHI; NAITO HIROYUKI 权利人:DAIICHI SEIYAKU CO 摘要:The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): n wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: n These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)- 1 piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-propene hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.
专利号:US-7972994-B2 优先权日:2003-12-17 标 题 :Methods for synthesis of encoded libraries
专利号:CN-116265466-A 优先权日:2021-12-16 标 题 :Synthesis of compounds that modulate use-dependent voltage-gated sodium channels
专利号:WO-2022133097-A1 优先权日:2020-12-17 标 题 :Synthesis of compounds that modulate use-dependent voltage-gated sodium channels 发明人:XIAO LI; MATHIEU STEVEN; COUMING VINCENT; PATIENCE DANIEL; KWOK ALBERT; ROSA PAGAN KEDWIN; SULEMAN ABID; JUSTICE DAVID; HUANG FEI; HWANG HEEJUN; JUNG JIYOUNG; HONG NA; HWANG JAEKWANG; JUNG DAHYE; HAHM BYOUNGIAE; KIM CHUNYOUNG; WALKER DONALD 权利人:BIOGEN MA INC; XIAO LI; MATHIEU STEVEN; COUMING VINCENT; PATIENCE DANIEL; KWOK ALBERT; ROSA PAGAN KEDWIN; SULEMAN ABID; JUSTICE DAVID; HUANG FEI; HWANG HEEJUN; JUNG JIYOUNG; HONG NA YEON; HWANG JAEKWANG; JUNG DAHYE; HAHM BYOUNGIAE; KIM CHUNYOUNG 摘要:The disclosure provides processes for preparing spiro derivatives, in particular (2R,5S)-7-methyl-2-[4-methyl-6-[4-(trifluoromethyl)-phenyl]pyrimidin-2-yl]-1,7- diazaspiro[4.4]nonan-6-one, as well as intermediates for use in said processes.
专利号:US-2004073054-A1 优先权日:2002-07-11 标 题 :New fluorous tagging and scavenging reactants and methods of synthesis and use thereof