专利号:US-5521310-A 优先权日:1992-10-07 标 题 :Process to obtain benzoxazines to be used for the synthesis of ofloxazine, levofloxazine and derivatives 发明人:CARRETERO GONZALVEZ JUAN-CARLO; VICIOSO SANCHEZ MERCEDES; GARCIA RUANO JOSE-LUIS 权利人:ETILO DERIVADOS 摘要:A process to obtain benzoxazines useful for the synthesis of Ofloxazine, Levofloxazine and derivatives. The benzoxacines (I) where Xb is an halogen and R 1 is H, alkyl or alkenyl of up to 6 atoms of C or aryl, can be obtained by means of cycling a compound of formula (II) through the reaction with triphenylphosphine and ethyl azodicarboxilate. The compounds of formula (II) can be obtained through the reaction of a compound (III) with an adequate epoxide. Through the use of the adequate chiral epoxide it is possible to obtain the enantiomerically desired intermediate and, therefore and selectively, it is possible to obtain the desired final product with the adequate enantiomeric form without the need to carry out a resolution stage. n The Compounds (I) are useful and key intermediates for the synthesis of the antimicrobials Oflixazine and Levofloxazine. ##STR1##
专利号:US-12391725-B2 优先权日:2016-06-22 标题:Method for production of novel galeterone analogs and uses thereof 发明人:NJAR VINCENT C O; PURANIK PURUSHOTTAMACHAR; MURIGI FRANCIS 权利人:NJAR VINCENT C O; PURANIK PURUSHOTTAMACHAR; MURIGI FRANCIS; NAT INSTITUTES OF HEALTH NIH U S DEPT OF HEALTH AND HUMAN SERVICES DHHS U S GOVERNMENT 摘要:Galeterone and its C-3 analogs are of substantial interest because of their multi-target anticancer activities, including AR and Mnk degrading activities. Provided are novel procedures for gram-scale, high-yield synthesis of C-3 analogs of galeterone, including 3β-(1H-imidazole-1-yl)-17-(1H-benzimidazole-1-yl)-androsta-5,16-diene (galeterone 3β-imidazole) and 3β-(pyridine-4-ylmethoxy)-17-(1H-benzimidazol-1-yl)androsta-5,16-diene (galeterone 3β-pyridine methoxylate).
专利号:US-6051711-A 优先权日:1997-10-24 标 题 :Synthesis of swainsonine salts 发明人:TROPPER FRANCOIS; SHAH RAJAN N; SHARMA PRADEEP 权利人:GLYCODESIGN INC 摘要:A method for synthesizing swainsonine salts and intermediates thereof comprising subjecting a compound of the formula I wherein R2 and R2' are the same or different and represent alkyl, halogen, alkenyl, alkoxy, cycloalkyl or aryl which may be substituted, to acid hydrolysis in the presence of a C1-4 alkanol to obtain a crystalline salt of swainsonine; and optionally, recrystallizing the swainsonine salt from a C1-4 alkanol. The reaction may be used in combination with one or more additional reaction steps.
专利号:US-5106750-A 优先权日:1988-08-30 标 题:Enantio- and regioselective synthesis of organic compounds using enol esters as irreversible transacylation reagents 发明人:WONG CHI-HUEY; WANG YI-FONG; HENNEN WILLIAM J; BABIAK KEVIN A; DYGOS JOHN H; NG JOHN S 权利人:SEARLE & CO 摘要:A process for irreversible regio- and stereoselective enzyme catalyzed acylation of alcohols using enol esters as acylating reagents is disclosed. The present invention permits the selective modification of hydroxyl group(s) of chiral and meso alcohols, including sugars, organometallics, and glycosides. The enol freed upon transesterification rapidly tautomerizes to the corresponding volatile aldehyde or ketone thereby preventing the reverse reaction from occurring.
专利号:US-5374745-A 优先权日:1990-03-29 标题 :Process for the synthesis of propargyl alcohols and their use for production of prostaglandin precursors 发明人:KLAR ULRICH 权利人:SCHERING AG 摘要:The invention relates to a process for the production of prostaglandin precursors of formula I ##STR1## as well as their enantiomers in which X is A--W or W--A, n A is a --C.tbd.C-- group, n W is a hydroxymethylene group, in which the OH group can be functionally modified by etherification or esterification, n D is a straight-chain or branched-chain alkylene group with 2-5 C atoms each or a ##STR2## group, n i s 1 to 3, n E is a --C.tbd.C-- group or a --CR 3 â•?CR 4 group with R 3 and R 4 each meaning a hydrogen atom or a C 1 -C 4 alkyl group, n R 1 is a hydrogen atom or a hydroxy group, which can be functionally modified as in W, n R 2 is a straight-chain or branched-chain alkyl group with 1-7 C atoms, characterized in that vinyl bromides of formula II ##STR3## in which Z means the group ##STR4## and R 1 , W, D, E and R 2 have the above-indicated meanings and hydroxy groups unprotected in R 1 and W or represented by an optionally substituted benzoyl radical, a C 1 -C 6 alkanoyl group, a tetrahydropyranyl radical, a tetrahydrofuranyl radical, a trialkylsilyl group or a diphenylalkylsilyl group each with alkyl meaning a C 1 -C 4 alkyl, are reacted with anhydrous cesium acetate in the presence of 18-crown6.
专利号:US-4794108-A 优先权日:1984-04-24 标题:1-carboxymethoxy acetidinones and their production 发明人:KISHIMOTO SHOJI; SENDAI MICHIYUKI; OCHIAI MICHIHIKO 权利人:TAKEDA CHEMICAL INDUSTRIES LTD 摘要:A 2-azetidinone derivative having a group of the formula wherein R1 and R2 are the same or different and each represents a hydrogen atom, alkyl, aryl or arylalkyl which may have a substituent at the 1-position and an amino group, at the 3-position, which may be acylated or protected, its salt or ester, and methods of producing the same, (1) a method comprising subjecting a 2-azetidinone derivative having a group of the formula wherein the symbols are as defined above at the 1-position and an amino group at the 3-position, its salt or ester to an acylation or protective-group introduction reaction, and (2) a method comprising reacting a 2-azetidinone derivative having a hydroxy group at the 1-position and an amino group, at the 3-position, which may be acylated or protected, or its salt with a compound of the formula wherein W is a halogen atom; other symbols are as defined above, its salt or ester. The above objective compounds are utilizable as excellent antimicrobial agents or as valuable intermediates for the synthesis of the same.
参考标题:Tert- Butyl Iodide Mediated Reductive Fischer Indolization Of Conjugated Hydrazones 作者:Yuta Ito,Masafumi Ueda,Norihiko Takeda,Okiko Miyata |发布日期:2016.2.18 摘要:Available N‐aryl Conjugated Hydrazones With Tert‐butyl Iodide Has Been Developed. In This Reaction, Tert‐butyl Iodide Is Used As Anhydrous Hi Source, And The Generated Hi Acts As A Brønsted Acid And A Reducing Agent. This Operationally Simple Method Allows Access To Various Indole Derivatives. Furthermore, The Procedure Can Be Applied To The Synthesis Of Biologically Active Compounds.