利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

79 条记录 (耗时 0.021 秒)

    Process for preparing anthracyclinones
    3.
    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 preparation of substituted benzofuran derivatives
    7.
    发明授权
    Process for the preparation of substituted benzofuran derivatives 失效
    取代苯并呋喃衍生物的制备方法

    公开(公告)号：US5459161A

    公开(公告)日：1995-10-17

    申请号：US78293

    申请日：1993-06-25

    申请人： Angelo Bedeschi ,  Walter Cabri ,  Ilaria Candiani ,  Silvia De Bernardinis ,  Marcello Marchi

    发明人： Angelo Bedeschi ,  Walter Cabri ,  Ilaria Candiani ,  Silvia De Bernardinis ,  Marcello Marchi

    IPC分类号： C07D307/84 ,  A61K31/34 ,  A61K31/343 ,  C07D307/79 ,  C07D307/83 ,  C07D405/12 ,  C07D451/04 ,  C07D451/14 ,  C07D453/02 ,  C07D453/06 ,  C07D455/02 ,  C07D471/08 ,  A61K31/40 ,  C07D207/08 ,  C07D307/78

    CPC分类号： C07D307/79 ,  C07D307/83 ,  C07D307/84 ,  C07D405/12 ,  C07D451/04 ,  C07D453/02 ,  C07D453/06 ,  C07D455/02 ,  C07D471/08 ,  Y02P20/55

    摘要： Substituted benzofuran derivatives of the formula (I): ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen or halogen and the other is, independently, an amino group or a C.sub.2 -C.sub.4 alkanoyl amino group; R.sub.3 is hydrogen; a linear or branched C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.2 -C.sub.4 alkoxycarbonyl group; halogen; or phenyl unsubstituted or substituted by a C.sub.1 -C.sub.4 alkyl group; A is a group --(CH.sub.2).sub.n -Het wherein Het is an optionally substituted heteromonocyclic or heterobicyclic ring containing one or two nitrogen atoms, and n is zero or an integer of 1 to 3; and the symbol ..... represents a single or double bond; may be prepared by a process comprising reacting a compound of formula II: ##STR2## in which L is a leaving group and R.sub.4 is hydrogen or a carboxy protecting group, with a compound of formula III;R'.sub.3 --C.dbd.C--R'.sub.3 IIIto obtain a compound of formula IV; ##STR3## which is then cyclized to obtain a compound of formula V; ##STR4## which is reacted with a compound of formula VI;H.sub.2 N--A VI.

    摘要翻译： PCT No.PCT / EP91 / 02512 Sec。 371日期：1993年6月25日 102（e）日期1993年6月25日PCT 1991年12月27日PCT PCT。 出版物WO92 / 12147 日本时间1992年7月23日。式（I）的取代苯并呋喃衍生物：其中R 1和R 2之一是氢或卤素，另一个独立地是氨基或C 2 -C 4烷酰基氨基; R3是氢; 直链或支链C 1 -C 4烷基，C 1 -C 4烷氧基或C 2 -C 4烷氧基羰基; 卤素; 或未被取代或被C 1 -C 4烷基取代的苯基; A是基团 - （CH 2）n -Het，其中Het是含有一个或两个氮原子的任选取代的杂单环或杂双环，且n为0或1至3的整数; 符号.....表示单键或双键; 可以通过包括使式II化合物：其中L是离去基团且R4是氢或羧基保护基的式II化合物与式III化合物反应来制备; R'3-C = C-R'3 III，得到式Ⅳ化合物; IV，然后将其环化以获得式V化合物; 其与式VI化合物反应; H2N-A VI。

    Process for preparing uracil derivatives
    8.
    发明授权
    Process for preparing uracil derivatives 失效
    制备尿嘧啶衍生物的方法

    公开(公告)号：US5286861A

    公开(公告)日：1994-02-15

    申请号：US928507

    申请日：1992-08-21

    申请人： Angelo Bedeschi ,  Walter Cabri ,  Ilaria Candiani ,  Tiziano Martinengo

    发明人： Angelo Bedeschi ,  Walter Cabri ,  Ilaria Candiani ,  Tiziano Martinengo

    IPC分类号： C07D239/553 ,  C07D239/54 ,  C07D239/60 ,  C07D239/545

    CPC分类号： C07D239/54 ,  C07D239/60

    摘要： The present invention relates to a novel process for preparing uracil derivatives useful as intermediates in the synthesis of uridines having antiviral or antitumor activity or useful as coadjuvants in antiviral therapy, characterized by converting a compound of the formula II into its mesylate derivative of the formula III which is the reduced to give the desired compound of the formula I: ##STR1## in which R.sub.1 is H, halogen, alkyl, aryl or aralkyl.

    摘要翻译： 本发明涉及一种制备尿嘧啶衍生物的新方法，其用作合成具有抗病毒或抗肿瘤活性的尿苷的中间体或用作抗病毒治疗中的辅佐剂，其特征在于将式（II）的化合物转化成式（II）的甲磺酸酯衍生物 III），其是还原得到所需的式（I）化合物，其中R 1是H，卤素，烷基，芳基或芳烷基。

    Process for the enzymatic separation of the optical isomers of racemic oxazolidinonic derivatives
    9.
    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
    10.
    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.