专利号:US-4707554-A 优先权日:1984-12-07 标 题 :Method of obtaining derivatives of 4β-/1'-alken-1'-yl/-2ξ,5α-dαβ-4,5,6,6α.beta. 发明人:ACHMATOWICZ BARBARA; DANIEWSKI ANDRZEJ R; MARCZAK STANISLAW; PANKOWSKI JACEK; WICHA JERZY 权利人:POLSKA AKADEMIA NAUK INSTYTUT 摘要:A new method has been disclosed for obtaining derivatives of 4β-/1'-alken-1'-yl/-2ξ,5â•?-dihydroxy-3,3aβ,4,5,6,6aβ-hexahydro-2H-cyclopenta [b] furane useful in the synthesis of prostaglandins or their analogs, and a method for obtaining new sulphonyl initial compounds of the general formula 4, in which Z denotes a hydrogen atom or a protective group, Y denotes a group of the formula â•?CHOZ 1 , in which Z 1 has the meaning stated for Z, whereby protective groups Z and Z 1 may be the same or different, and Ar denotes optionally a substituted aryl group. n In the method according to the invention the new sulphonyl derivative of the general formula 4 is alkylated with an electrophilic agent comprising: carbonyl derivatives, oxiranes and halohydrins or their derivatives; the alkylation product is transformed into derivatives of 4β-/1'-alken-1'-yl/-2ξ,5α-dihydroxy-3,3aβ,4,5,6,6a.beta.-hexahydro-2H-cyclopenta[b] furane in reactions which ensure obtaining a double bond C 13 -C 14 . n New sulphonyl initial compounds of the general formula 4 are obtained from lactone of the general formula 11, in which Z has the above stated meaning and L° denotes a leaving group, which is transformed into a sulphide; the obtained lactone-sulphide is reduced to lactol, and thereafter lactol-sulphide is oxidized to te sulphonyl derivative.
专利号:US-4927963-A 优先权日:1989-04-28 标题 :Novel processes for the synthesis of certain bicyclo(4.2.0)octane derivatives with valuable therapeutic properties 发明人:WALKER KEITH A M; KERTESZ DENIS J 权利人:SYNTEX INC 摘要:A process for preparing compounds represented by the formula ##STR1## wherein: X is hydrogen or lower alkoxy; n Y is hydrogen, exo-(lower alkyl) or endo-(lower alkyl); n n is an integer from 2-4; n R 2 is hydrogen or methyl; and n R 3 is linear or branched alkyl, ##STR2## --(CH 2 ) m -phenyl or --CH 2 O-phenyl; in which any phenyl may be optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen, and n a is an integer of 0, 1 or 2; n b is an integer of 3-7; n m is an integer of 0, 1 or 2, n as a mixture or separately in a sequence starting from an epoxide represented by the formula ##STR3## and processes for making the novel intermediates.
专利号:US-3910965-A 优先权日:1971-11-29 标 题 :Process for the preparation of 2-formylcyclopentane derivatives 发明人:SAKAI KIYOSHI; KOJIMA KOICHI; YUSA TAKASHI; KATANO HAMAKO 权利人:SANKYO CO 摘要:A process for the preparation of 2-formylcyclopentane derivatives having the formula WHEREIN A represents a straight or branched alkylene group having 1*8 carbon atoms, Z represents cyano group, carbamoyl group, carboxyl group or an alkoxycarbonyl group having 1*6 carbon atoms in the alkyl moiety and R represents a tetrahydropyranyl group or an alkoxyalkyl group having 1*6 carbon atoms in each alkyl moiety or its optical isomer or the racemic mixture thereof which comprises conntacting a 2hydroxymethylcyclopentane derivative having the formula WHEREIN A, Z and R are the same as above or its optical isomer or the racemic mixture thereof with an oxidizing agent in the presence of a solvent at the temperature ranging from -30*C to room temperature. The 2-formylcyclopentane derivatives are useful as intermediates for synthesis of prostaglandin F Alpha .
专利号:US-6307050-B1 优先权日:2000-08-29 标题:Method of synthesizing flosequinan from 4-fluoroanthranilic acid 发明人:KWIATKOWSKI STEPHAN; SIDDIDQUI MAYA; EISENBERG RODNEY; MUKHOPADHYAY SUDARSAN; LAWRENCE LOWELL JEFFRY; MOBLEY STEVEN G 权利人:R T ALAMO VENTURE I LLC 摘要:A high-yield, 4-step synthesis for flosequinanstarting with 4-fluoroanthranilic acid comprising cyclization with phosgene to create an intermediate -A, followed by methylation to create an intermediate -B, then by reaction with dimsyl sodium to create an intermediate -C, then by reaction with triethyl orthoformate in the presence of piperdine and acetic acid to give flosequinan. The overall yield of the disclosed process is greater than about 16%.
专利号:PL-104614-B1 优先权日:1973-12-14 标题:METHOD OF MAKING NEW POLPRODUCTS FOR THE SYNTHESIS OF NEW OMEGA-PENTANORPROSTAGLANDINS
专利号:US-4476315-A 优先权日:1982-04-30 标 题:Nucleophilic substitution process 发明人:STAHLY G PATRICK; STAHLY BARBARA C 权利人:ETHYL CORP 摘要:Nitroarylacetic acid esters are prepared by reacting a nitroaromatic compound which is devoid of halogen on the aromatic ring carrying a nitro group with an alpha,alpha-disubstituted acetic acid ester in an inert solvent and in the presence of a base so that the ester undergoes a nucleophilic substitution on an unsubstituted ring carbon of the nitroaromatic compound during which an alpha-substituent functions as a leaving group. Nitrobenzene acetic acids and their esters are useful intermediates for the synthesis of pharmaceuticals.