CAS: 7051-34-5; (Bromomethyl)Cyclopropane

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CAS号2516-33-8 环丙基甲醇 | CAS号756488-62-7 Benzamide,N-(cy... | CAS号5911-08-0 氯甲基环丙烷 | CAS号42392-28-9 cyclobutane car... | CAS号7789-60-8 三溴化磷 | CAS号931-82-8 cyclopropylmeth... | CAS号186581-53-3 重氮甲烷 | CAS号106-95-6 烯丙基溴 | CAS号75-09-2 二氯甲烷 | CAS号40487-93-2 环丙甲肼 | CAS号33574-02-6 (碘甲基)环丙烷 | CAS号3710-30-3 1,7-辛二烯 | CAS号45892-60-2 1-but-3-enyl-2-... | CAS号605-39-0 2,2'-二甲基联苯 | CAS号91130-35-7 1-(cyclopropylm... | CAS号20242-36-8 5-[1-(cycloprop... | CAS号19444-23-6 2-羟基-2-甲基丙酸苄酯 | CAS号111-66-0 1-辛烯 | CAS号2511-91-3 1-cyclopropylpentane

环丙乙酸置于碘苯二乙酸,Potassium Bromide体系中,用 二氯甲烷 作为反应溶剂,以56%的收率获得产物溴甲基环丙烷
参考文献:高价碘试剂对立体受阻羧酸的脱羧溴化反应
标题:高价碘试剂对立体受阻羧酸的脱羧溴化反应
摘要:立体受阻的三维(3D)烷基卤化物是各种反应的有希望的前体;但是,它们难以通过常规反应合成.我们提供了使用市售的(diacetoxyiodo)苯和溴化钾(自然界中最稳定和最便宜的溴源之一)对位阻3D脂肪族羧酸进行脱羧溴化的高效实用方法.本方法的特点是不含金属/ Br 2无体系,温和的反应条件,在室温下空气中一锅操作,广泛的官能团相容性和克级合成能力.这种高效的反应可以以高收率或高收率干净地将各种羧酸(高度紧张/天然存在/与药物相关的支架的最便宜和最容易获得的来源)转化为相应的烷基溴化物.
DOI:10.1021/acs.Oprd.0C00130

专利信息

专利号:US-5668285-A
优先权日:1986-10-31
标 题 :Total synthesis of northebaine, normophine, noroxymorphone enantiomers and derivatives via N-Nor intermediates
发明人：RICE KENNER CRALLE; NEWMAN AMY HAUCK
权利人:US HEALTH
摘要:The invention involves a method of making key intermediates useful in the synthesis of many opiate narcotics and antagonists and agonists; and the non-opiate enantiomers thereof which have potent antitussive properties. The synthesis starts from either the natural or unnatural enantiomer of nordihydrocodeinone and produces 8, 14-dihydronorthebaine, the diketal of 7-bromonordihydrocodeinone, northebaine, norcodeinone diketal and 14-hydroxynorcodeinone intermediates without the necessity of leaving the N-nor structure. The syntheses have fewer steps than previous methods, and also have high yields.

专利号:EP-0496830-B1
优先权日:1989-10-16
标 题 :Total synthesis of northebaine, normorphine, noroxymorphone enantiomers and derivatives via n-nor intermediates
发明人：RICE KENNER CRALLE; NEWMAN AMY HAUCK
权利人:US HEALTH
摘要:Families of antagonist-agonists and opiate narcotics are produced from norhydrocodeinone. In a preferred embodiment, norhydrocodeinone is refluxed with sulfosalicyclic dimethylketal and delta-6-enol ether derivatives and is then converted entirely to the ether by the addition of dry tetrahydrofuran simultaneously with the removal of the thus produced ether. The ether is then reacted with methanesulfonic acid and N-bromoacetamide to form the hydrobromide salt of the 7-bromodimethylketal derivative. From this derivative, a variety of products can be derived, including the novel further intermediate 14 hydroxynorcodeinone. The present invention enables derivation using a starting material which, unlike the starting materials of prior art processes, is available in the natural (-) or synthetic (+) form. Thus, the method of the present invention provides the only known route for the synthesis of (+) forms of various derivatives and intermediates, such as (+)-7-bromo-dimethylketal nordihydrocodeinone.

专利号:US-11905296-B2
优先权日:2020-01-27
标题:Process for the synthesis of buprenorphine
发明人：ZINSER HARTMUT; DANIELYAN TAMAR; GRIGORYAN MERI; GHARIBYAN MARIAM; MOVSISYAN MIKAYEL; NERKARARYAN KRISTINE
权利人:AZAD PHARMA AG
摘要:The present invention relates to a novel route of synthesis for the opioid receptor antagonist Buprenorphine or a pharmaceutically acceptable salt thereof, starting from thebaine, wherein the route comprises the reaction of thebaine with a dienophile; forming an alkylated reaction product by reaction with a Grignard-reagent; formation of an cyanamide; deprotection of the cyanamide- and the phenolic-oxygen-moiety, wherein the cleavage of one or both groups is performed in the presence of an alkali or alkaline earth sulfide; followed by derivatization with a cyclopropyl-halogen and hydrogenation to yield Buprenorphine.

专利号:US-9388147-B2
优先权日:2009-11-13
标题 :Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis
发明人：MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TIMONY GREGG ALAN; BROOKS JENNIFER L; PEACH ROBERT; SCOTT FIONA LORRAINE; HANSON MICHAEL ALLEN
权利人:RECEPTOS INC; CELGENE INTERNAT II SÃ?RL
摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.

专利号:US-2014309424-A1
优先权日:2011-06-30
标题:Direct synthesis of 18f-fluoromethoxy compounds for pet imaging and the provision of new precursors for direct radiosynthesis of protected derivatives of o-([18f] fluoromethyl) tyrosine
发明人：BRUMBY THOMAS; GRAHAM KEITH; KRUGER MARTIN
权利人:BRUMBY THOMAS; GRAHAM KEITH; KRUGER MARTIN; PIRAMAL IMAGING SA
摘要:The invention describes novel direct synthesis methods for converting a precursor into a PET-tracer with a 18 F-fluoromethoxy-group. The invention is also directed to novel and stable precursors for the direct radiosynthesis of protected derivatives of O—([ 18 F]Fluoromethyl)tyrosines.

专利号:US-12275733-B2
优先权日:2016-11-07
标 题:Substituted pyrido[3,4-b]indoles for the treatment of cartilage disorders
发明人：GRETZKE DIRK; RITZELER OLAF; HEINELT UWE; WEHNER VOLKMAR; SCHMIDT FRIEDEMANN
权利人:SANOFI SA
摘要:The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula (I), in which A, E, G, R1 to R6 and R10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.