CAS: 6981-18-6; 5-(4,5-Dimethoxy-2-Methylbenzyl)Pyrimidine-2,4-Diamine

上下游产品

CAS号593-85-1 碳酸胍 | CAS号7520-75-4 cinnamonitrilee | CAS号124-46-9 carbonic acid; ... | CAS号494-99-5 3,4-二甲氧基甲苯 | CAS号54236-98-5 2,4-Diamino-5-m... | CAS号22002-45-5 3-溴-4-甲氧基甲苯 | CAS号7721-62-2 4,5-二甲氧基-2-甲基苯甲醛 | CAS号39800-76-5 3-methoxy-2-(me... | CAS号50-01-1 盐酸胍 | CAS号124-41-4 甲醇钠

3,4-二甲氧基甲苯置于sodium Methylate,三氯氧磷体系中,用 甲醇,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 0.5H,反应生成 奥美普林
参考文献:一种奥美普林的合成方法
标题:一种奥美普林的合成方法
摘要:本发明提供了一种奥美普林的合成方法,该方法包括下列步骤:将对甲苯酚与碳酸二甲酯进行酚羟基甲基化反应制得化合物ⅰ;在醋酸酐‑硝酸体系下将化合物ⅰ与溴化钾进行溴代反应制得化合物ⅱ;以氯化亚铜为催化剂,化合物ⅱ与甲醇钠的甲醇溶液进行甲氧基化反应制得化合物ⅲ;化合物ⅲ与vha试剂进行甲酰化反应制得化合物ⅳ;化合物ⅳ通过与甲醇钠,丙烯腈的甲醇溶液反应制得化合物ⅴ;化合物ⅴ先经碱催化异构化到烯醚结构,再与甲醇加成,直接与胍缩合环化,最终制得化合物ⅵ,即最终产物奥美普林.本发明克服了上述现有技术中的不足,提供了一种工艺简单,起始原料易得,收率高,生产成本低的奥美普林合成方法.

专利信息

专利号:US-4216319-A
优先权日:1976-06-09
标题:Synthesis of 2,4-diamino-5-benzylpyrimidines using benzyl cyanoacetal intermediates
发明人：SWARINGEN ROY A JR; YEOWELL DAVID A
权利人:BURROUGHS WELLCOME CO
摘要:Benzyl cyanoacetals of formula: ##STR1## wherein R 1 , R 2 and R 3 are the same or different and each is a halogen or a hydrogen atom, an alkoxy group, an alkyl group, or a dialkylamino group; R 4 is an alkoxycarbonyl group, or an aldehyde group; and R 5 is an alkyl group; the alkyl or alkoxy groups each having from 1 to 4 carbon atoms, and their use as intermediates in the preparation of antibacterial 2,4-diamino-5-benzylpyrimidines. They are prepared from a reaction between an orthoester and an α-substituted-β-benzylpropionitrile and then the resulting cyanoacetal is converted to the benzylpyrimidine by reaction with guanidine.

专利号:US-9439423-B2
优先权日:2007-10-29
标 题 :Antiparasitic agent for fish and method of controlling proliferation of fish parasites
发明人：KAWANO FUMI; HIRAZAWA NORITAKA
权利人:KAWANO FUMI; HIRAZAWA NORITAKA; NIPPON SUISAN KAISHA LTD
摘要:An antiparasitic agent for fish includes an inhibitor of folate synthesis and/or an inhibitor of folate activation as the active substance(s). A combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is disclosed. Sulfonamide is disclosed as suitable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist are disclosed as suitable inhibitors of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is effective against fish parasites belonging to the ciliate group.

专利号:US-4151196-A
优先权日:1975-06-26
标题 :Cyano-enol ethers
发明人：ROSEN PERRY
权利人:HOFFMANN LA ROCHE
摘要:The present invention relates to a new synthesis for the preparation of 5-(substituted benzyl)-2,4-diamino-pyrimidines, including new pyrimidine derivatives. More particularly, a new synthesis of ormetoprin, diaveridine and related compounds, including novel derivatives, is disclosed. The synthesis involves the condensation of a substituted benzene and an acrylonitrile derivative to directly give enol ether intermediates, which upon subsequent reaction by known techniques with guanidine, provides the desired 5-(substituted benzyl)-2,4-diamino-pyrimidines, including novel compounds. The pyrimidine end products are useful as potentiators of sulfonamides and as antibacterial agents.

专利号:US-9265777-B2
优先权日:2009-04-27
标题 :Antiparasitic agent for fish and method of controlling proliferation of fish parasites
发明人：KAWANO FUMI; HIRAZAWA NORITAKA
权利人:KAWANO FUMI; HIRAZAWA NORITAKA; NIPPON SUISAN KAISHA LTD
摘要:A method of controlling proliferation of fish parasites comprising the administration of 1 to 50 mg/kg fish body weight/day of an inhibitor of folate synthesis and/or an inhibitor of folate activation to fish continuously for 1 to 2 weeks. Using a combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is preferable, and a sulfonamide is preferable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist, etc., can be used as the inhibitor of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is particularly effective against parasites belonging to the ciliate group among fish parasites.

专利号:WO-2009056955-A1
优先权日:2007-10-30
标题 :Amine-bearing phospholipids (abps), their synthesis and use
发明人：ZUMBUEHL ANDREAS
权利人:UNIV BASEL; ZUMBUEHL ANDREAS
摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.

专利号:US-9907753-B2
优先权日:2010-03-19
标 题 :Lipid vesicle compositions and methods of use
发明人：IRVINE DARRELL J; MOON JAEHYUN
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The invention provides delivery systems comprised of stabilized multilamellar vesicles, as well as compositions, methods of synthesis, and methods of use thereof. The stabilized multilamellar vesicles may comprise prophylactic, therapeutic and/or diagnostic agents.