1,1'-氧基二(环己烷)置于溴,双氧水体系中,用 二氯甲烷,水 用作溶剂,化学反应 5.0H,以93%的收率获得环己酮 参考文献:Amati,Alessandro; Dosualdo,Gabriele; Zhao,Lihua,Organic Process Research And Development,1998,Vol. 2,# 4,P. 261-269 标题:Amati,Alessandro; Dosualdo,Gabriele; Zhao,Lihua,Organic Process Research And Development,1998,Vol. 2,# 4,P. 261-269
专利信息
专利号:US-9527800-B2 优先权日:2013-10-29 标 题:Process for total synthesis of venlafaxine 发明人:CHAVAN SUBHASH PRATAPRAO; PAWAR KAILASH PRALHAD 权利人:COUNCIL SCIENT IND RES 摘要:There is a need for short, resolution free asymmetric process for synthesis of one isomer of venlafaxine, (−)-venlafaxine. The invention provides a novel, short process of synthesis of (−)-venlafaxine, with yield greater than 50% and ee>99%. This process can be used for racemic synthesis of venlafaxine with overall yield 65%.
专利号:US-4354972-A 优先权日:1981-06-29 标 题 :Synthesis of steroids 发明人:KAISER EMIL T 权利人:KAISER EMIL T 摘要:This invention relates to the synthesis of steroids which are useful for their biological activity or which may be converted to steroids which have such activity. These syntheses include the steroid compounds and processes for their preparation. n An object of the invention is to provide syntheses which are applicable to materials which are readily available in good supply for converting such materials to steroids which are useful and desirable in the manufacture of pharmaceutical products. n More particularly, I have sought to discover processes and intermediate compounds useful in the synthesis of 24, 25-dihydroxycholesterol from hyodeoxycholic acid or lithocholic acid which are constituents of, and readily available from, animal bile.
专利号:US-3852307-A 优先权日:1972-04-25 标 题 :Synthesis of zearalanone and related compounds 发明人:URRY W; MULLENBACH G 权利人:COMMERCIAL SOLVENTS CORP 摘要:WHEREIN X is an integer having a value from 0 to 6 inclusive and Y is an integer having a value from 3 to 8 inclusive. It also provides for new methods of making compounds useful in the synthesis of zearalanone and related compounds. The compounds 6-acetoxyhexanoic acid; 2-(5-hexenoyl)cyclohexanone; 7-keto-11-dodecenoic acid; 2-hydroxyethyl 7-keto11-dodecenoate ethylene ketal; N,N-dimethyl 7-keto-11dodecenamide ethylene ketal; 7-keto-11-dodecenal ethylene ketal; 9-keto-2,13-tetradecadienic acid ethylene ketal; 2-hydroxyethyl 9-keto-2,13-tetradecadienoate ethylene ketal; the sodium salt of ethyl 6-(6-keto-10-undecenyl)- Beta -dihydroresorcylate ethylene ketal; ethyl 3-bromo-6-(6-keto-10-undecenyl)- Beta dihydroresorcylate ethylene ketal; ethyl 6-(6-keto-10-undecenyl)Beta -resorcylate ehtylene ketal; ethyl 6-(6-keto-10-undecenyl)Beta -resorcylate ethylene ketal dibenzyl ether; ethyl 6-(6keto-10-hydroxyundecyl)- Beta -resorcylate ethylene ketal dibenzyl ether; and 6-(10-hydroxy-6-keto-undecyl)- Beta resorcylic acid dibenzyl ether are disclosed. Methods for preparing these compounds are also disclosed. This invention provides a new synthesis for zearalanone and for related compounds having more or fewer carbon atoms in the nonaromatic ring than does zearalanone, which related compounds and zearalanone are represented by the formula
专利号:EP-0439404-B1 优先权日:1990-01-25 标题 :Preparation of 2-(2'-thienyl) alkylamines and derivatives thereof and synthesis of 4,5,6,7- thieno [3,2-c] pyridine derivatives therefrom 发明人:KHATRI HIRALAL N; DEHOFF BRADLEY S 权利人:SANOFI SA 摘要:An improved process for the synthesis of 2-(2 min -thienyl)ethylamine from suitably functionalized derivatives of 2-(2 min -thienyl)ethanol employing ammonia gas in the presence of a metal salt or liquid ammonia and alkyl ketone as a solvent. The 2-(2 min -thienyl)ethylamine produced by this process is advantageously converted to the carbamic acid salt, which is suitably reconverted to 2-(2 min -thienyl)ethylamine, a useful intermediate in the synthesis of ticlopidine.
专利号:US-7612210-B2 优先权日:2005-12-05 标题:Process for selective synthesis of enantiomers of substituted 1-(2-amino-1-phenyl-ethyl)-cyclohexanols 发明人:MAHANEY PAIGE ERIN; ANTANE MADELENE MIYOKO; SUN JERRY SHUNNENG 权利人:WYETH CORP 摘要:A process for the enantioselective synthesis of an (S)- or (R)-1-[2-dimethylamino)-1-(methoxyphenyl)ethyl]cyclohexanol and analogues or salt thereof are described. The method involves the steps of (a) reacting an (S) or (R) 4-benzyloxazolidinone with a mixed anhydride of a methyoxyphenylacetic acid under conditions which form a oxazolidinone, (4S)- or (4R)-4-benzyl-3-[methyoxyphenyl]acetyl]-oxazolidin-2-one, (b) treating the (4S)- or (4R)-4-benzyl-3-[(methoxyphenyl)acetyl]-1,3-oxazolidin-2-one with an aprotic amine base and titanium chloride in a chlorinated solvent under conditions which permit formation of the corresponding anion, (c) mixing the corresponding anion with titanium chloride and cylcohexanone under conditions which permit an aldol reaction to form the corresponding (4S)- or (4R)-4-benzyl-3-[(2R)-2-(1-hydroxycyclohexyl)-2-(methoxyphenyl)acetyl]-1,3-oxazolidin-2-one,(d) hydrolyzing the (4S)— or (4R)-4-benzyl-3-[(2R)-2-(1-hydroxycyclohexyl)-2-(methoxyphenyl)acetyl]-1,3-oxazolidin-2-one to form a chiral acid (2S or 2R)-(1-hydroxycyclohexyl)-methoxyphenyl)acetic acid, (e) coupling the chiral phenylacid to a secondary amine to form an amide, and (f) reducing the amide to form an (S) or (R) 1[2-dimethylamino)-1-(methoxyphenyl)ethyl]cyclohexanol or a salt thereof.
专利号:US-6995289-B2 优先权日:2000-08-02 标题 :Process for synthesis of alpha, beta-unsaturated ketones 发明人:PATEL IAN; HOPES PHILIP 权利人:ASTRAZENECA AB 摘要:A method for the synthesis of an α,β-unsaturated ketone useful for making substituted 1,4-dihydropyridines is described by reacting an aldehyde with pyrrolidine and then adding a ketone followed by trifluoroacetic acid at low temperature. The synthesis is used in a process for making substituted 1,4-dihydropyridines wherein a vinylogous amide is prepared by reacting a 1,3-cyclohexanedione with a phenylethylamine. The α,β-unsaturated ketone can be reacted with a vinylogous amide to form a 1,5-diketone which can be converted to a substituted 1,4-dihydropyridine.
参考标题:Organocatalyzed Kabbe Condensation Reaction For Mild And Expeditious Synthesis Of 2,2‐dialkyl And 2‐spiro‐4‐chromanones 作者:Naval P. Kapuriya,Jasmin J. Bhalodia,Mrunal A. Ambasana,Rashmi B. Patel,Atul H. Bapodra 摘要:An Expeditious Kabbe Condensation Reaction For The Synthesis Of 2,2‐dialkyl And 2‐spiro‐chroman‐4(1H)‐ones Has Been Developed Using Pyrrolidine‐butanoic Acid In Dmso As Bifunctional Organocatalyst. Unlike Existing Methods, This Reaction Proceeds At Room Temperature With High Yields, Rendering It An Attractive Method To Synthesize A Vast Variety Of Privileged 4‐chromones.