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    Process for preparing anthracyclinones
    4.
    发明授权
    Process for preparing anthracyclinones 失效
    制备蒽醌的方法

    公开(公告)号：US5180758A

    公开(公告)日：1993-01-19

    申请号：US743373

    申请日：1991-08-26

    申请人： Walter Cabri ,  Ilaria Candiani ,  Silvia De Bernardinis ,  Franco Francalanci

    发明人： Walter Cabri ,  Ilaria Candiani ,  Silvia De Bernardinis ,  Franco Francalanci

    IPC分类号： B01J27/128 ,  B01J31/12 ,  C07B61/00 ,  C07C46/00 ,  C07C49/423 ,  C07C49/727 ,  C07C50/36 ,  C07C50/38

    CPC分类号： C07C46/00 ,  Y02P20/55

    摘要： 4-substituted anthracyclinones of general formula (I): ##STR1## wherein R represents a hydrogen atom or a COOR.sub.1 group in which R.sub.1 may be a hydrogen atom or an optionally substituted C.sub.1 -C.sub.10 alkyl group, which are intermediates in the preparation of antitumor anthracycline glycosides, are prepared by:(i)(a) reacting a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V): ##STR2## wherein R' represents an alkyl group having from 1 to 10 carbon atoms optionally substituted by one or more halogen atoms or an aryl group optionally substituted by halogen, alkyl, alkoxy or nitro, in a reducing environment with a catalytic amount of a compound of formula (VIII):ML.sub.n L'.sub.m wherein M represents a transition metal atom, L and L', which may be the same or different, each represent an anion or a neutral molecule and n and m may vary from 0 to 4, such as to obtain a compound of formula (VII): ##STR3## wherein R represents hydrogen; or (b) carbonylating a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V) as defined above, with carbon monoxide in the presence of a nucleophile R.sub.1 OH wherein R.sub.1 is as defined above, an organic or inorganic base and as catalyst a compound of formula (VIII) as defined above, such as to obtain a compound of formula (VII) as shown above wherein R represents a COOR.sub.1 group; and(ii) introducing an .alpha.-hydroxy group at the 7-position and removing the 13-oxo protecting group by acid hydrolysis from the resultant compound of formula (VII).

    Process for the enzymatic separation of the optical isomers of racemic oxazolidinonic derivatives
    6.
    发明授权
    Process for the enzymatic separation of the optical isomers of racemic oxazolidinonic derivatives 失效
    外消旋恶唑烷酮衍生物的光学异构体的酶分离方法

    公开(公告)号：US4933290A

    公开(公告)日：1990-06-12

    申请号：US137721

    申请日：1987-12-24

    申请人： Pietro Cesti ,  Daniele Bianchi ,  Franco Francalanci ,  Walter Cabri

    发明人： Pietro Cesti ,  Daniele Bianchi ,  Franco Francalanci ,  Walter Cabri

    IPC分类号： C12P17/14 ,  C12P41/00

    CPC分类号： C12P17/14 ,  C12P41/004

    摘要： There is disclosed a process for the biotechnological resolution, by enzymatic esterification of the corresponding racemic mixture of the S(+) and R(-) optical isomers of the oxazolidinonic compounds having formula (I): ##STR1## wherein R represents a, linear or branched, C.sub.1 -C.sub.8 alkyl group, which process is characterized in that, the racemic 3-alkyl-5-hydroxymethyl-oxazolidin-2-one derivative of formula (I) is reacted with an esterifying compound, selected from esters having formula (III): ##STR2## wherein R represents a, linear or branched, C.sub.1 -C.sub.10 alkyl or alkenyl group and R" represents a linear or branched, C.sub.1 -C.sub.4 alkyl, alkenyl group, a haloalkyl (chlorine, bromine) group or a diacyl glycerolic group or from acids having formula (IV):R'"--COOH (IV)wherein R'" represents a, linear or branched, C.sub.1 -C.sub.20 alkyl or alkenyl group or from anhydrides having formula (V): ##STR3## wherein R.sup.IV represents a, linear or branched, C.sub.1 -C.sub.6 alkyl group, in the presence of an enzyme, immobilized on a porous carrier, capable of giving rise selectively to the esterification reaction of the R(-) isomer, while leaving the S(+) isomer substantially unchanged, which latter is then separated according to known techniques.

    Process for the enzymatic separation of the optical isomers of racemic .alpha.-alkyl-substituted primary alcohols
    7.
    发明授权
    Process for the enzymatic separation of the optical isomers of racemic .alpha.-alkyl-substituted primary alcohols 失效
    用于酶分离外消旋的α-烷基取代的伯醇的光学异构体的方法

    公开(公告)号：US4980291A

    公开(公告)日：1990-12-25

    申请号：US307913

    申请日：1989-02-09

    申请人： Daniele Bianchi ,  Pietro Cesti ,  Franco Francalanci ,  Walter Cabri

    发明人： Daniele Bianchi ,  Pietro Cesti ,  Franco Francalanci ,  Walter Cabri

    IPC分类号： C12P7/62 ,  C12P41/00

    CPC分类号： C12P41/004 ,  C12P7/62

    摘要： Biotechnological resolution by means of enzymatic transesterification of the relevant racemic mixture of the optical isomers of .alpha.-alkyl-substituted primary alcohols having the formula (I): ##STR1## wherein: R represents a linear or branched (C.sub.1 -C.sub.20)-alkyl or alkenyl group or an aryl group, also substituted or condensed with other groups, in particular a group of formula (II) or (III): ##STR2## wherein: R.sup.ii represents a (C.sub.1 -C.sub.8)-alkyl group, a (C.sub.1 -C.sub.4)-alkenyl group, an alkoxy, phenyl, phenoxy, benzoyl, or heterocyclic group;R.sup.iii represents a hydrogen or halogen atom;R.sup.iv represents a (C.sub.1 -C.sub.4)-alkyl group, and whereinR.sup.i represents a (C.sub.1 -C.sub.4)-alkyl group either equal to, or different from, R,in the presence of an enzyme either free or immobilized on a support capable of selectively causing the S isomer to be esterified, with the R isomer being left substantially unchanged, said isomers being then separated according to techniques known from the prior art. The process is used in the synthesis of antiinflammatory agents.

    Process for the preparation of penems
    8.
    发明授权
    Process for the preparation of penems 失效
    制备青铜器的过程

    公开(公告)号：US5364768A

    公开(公告)日：1994-11-15

    申请号：US940784

    申请日：1992-09-04

    申请人： Maria Altamura ,  Franco Francalanci ,  Marcello Marchi

    发明人： Maria Altamura ,  Franco Francalanci ,  Marcello Marchi

    IPC分类号： C07D499/88 ,  C12P37/00

    CPC分类号： C07D499/88

    摘要： An in vitro process for preparing 6((1R)-hydroxyethyl) penem acids by hydrolyzing the carboxylic ester derivative thereof using an enzyme capable of selectively hydrolyzing the ester group at the 3-position of the carboxylic acid ester using an esterase, acylase or lipase enzyme, wherein the enzymatic hydrolysis is effected at a pH in the range of from 5 to 8 and at a temperature in the range of 20.degree. C. to 40.degree. C.

    摘要翻译： 通过使用能够使用酯酶，酰基转移酶或脂肪酶选择性水解羧酸酯的3位的酯基的酶来水解其羧酸酯衍生物来制备6（（1R） - 羟乙基）青霉烯酸的体外方法 酶，其中酶水解在5至8范围内的温度和20℃至40℃的温度下进行。

    Process for the preparation of esters or salts of aromatic or etheroaromatic acids
    10.
    发明授权
    Process for the preparation of esters or salts of aromatic or etheroaromatic acids 失效

    公开(公告)号：US4537970A

    公开(公告)日：1985-08-27

    申请号：US560228

    申请日：1983-12-12

    申请人： Marco Foa ,  Franco Francalanci ,  Andrea Gardano ,  Elena Bencini

    发明人： Marco Foa ,  Franco Francalanci ,  Andrea Gardano ,  Elena Bencini

    IPC分类号： C07C67/36 ,  B01J31/00 ,  B01J31/20 ,  C07B31/00 ,  C07B41/12 ,  C07B61/00 ,  C07C51/10 ,  C07C67/00 ,  C07C69/76 ,  C07D213/80 ,  C07D307/68 ,  C07D333/38 ,  C07D239/02

    CPC分类号： C07D213/80 ,  C07C51/10 ,  C07D307/68

    摘要： This invention relates to the preparation of esters or salts of aromatic or etheroaromatic acids having formula Y--Ar--CO--OR (I), where:Ar represents an aromatic group constituted by one or more benzene rings, optionally condensed, or an etheroaromatic nucleus optionally condensed with one or more benzene rings;Y represents from zero to more substituents, equal or different, chosen among a halogen; an alkyl group having up to 6 carbon atoms; an alkoxy group having up to 5 carbon atoms; an ester group --COOR', where R' contains up to 5 carbon atoms; a hydroxyl group; a phenyloxy group, optionally substituted with groups inert under reaction conditions; a trifluoromethyl group; a nitrile group; an amidic group (--CONH.sub.2); an acetamidic group (--NH--CO--CH.sub.3); or an acyl group --CO--R", where R" represents a hydrocarbon group having up to 8 carbon atoms;R represents an alkyl group R.sub.1 having up to 5 carbon atoms or an alkali metal or alkaline earth metal M.These esters and salts (I) are obtained by reaction of a halide Y--Ar--X (II), where Ar and Y have the hereinabove defined meanings, while X is Cl, Br or I, with carbon monoxide, in an alcoholic solvent R.sub.1 OH (where R.sub.1 is an alkyl group having up to 5 carbon atoms) at atmospheric pressure and at temperatures ranging between -10.degree. and 60.degree. C. in the presence of an acidity-acceptor compound and of a catalyst constituted by a cobalt complex having formula (III):Z--Co(CO).sub.4 (III)where Z is a group chosen among CH.sub.3 ; CH.sub.2 F; CHF.sub.2 ; CF.sub.3 ; CH.sub.2 --CN; CH.sub.2 --COOR'", where R'" is an alkyl group having up to 8 carbon atoms or a benzene group, the latter optionally substituted with groups inert under reaction conditions; CH.sub.2 Ar', where Ar' is an aromatic group constituted by from one to three benzene rings optionally condensed and optionally substituted with groups inert under the reaction conditions, in particular with electron-attractor groups.