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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 preparation of substituted benzofuran derivatives
    8.
    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。