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    IMPROVED PROCESS FOR THE PREPARATION OF 2-SUSTITUTED-2-(6-(SUBSTITUTED)-7-METHYLBENZO[D][1,3]DIOXOL-4-YL)ACETIC ACID DERIVATIVES
    37.
    发明申请
    IMPROVED PROCESS FOR THE PREPARATION OF 2-SUSTITUTED-2-(6-(SUBSTITUTED)-7-METHYLBENZO[D][1,3]DIOXOL-4-YL)ACETIC ACID DERIVATIVES 审中-公开
    制备2-巯基-2-（6-（取代的）-7-甲基苯并[D] [1,3]二氧代-4-基）乙酸衍生物的改进方法

    公开(公告)号：WO2013190571A1

    公开(公告)日：2013-12-27

    申请号：PCT/IN2013/000381

    申请日：2013-06-19

    申请人： NATCO PHARMA LIMITED

    发明人： MUDDASANI, Pulla Reddy ,  CHINTALAPUDI, Manikumar ,  NANNAPANENI, Venkaiah Chowdary

    IPC分类号： C07D317/64 ,  C07C15/02

    CPC分类号： C07D317/64 ,  C07C43/23 ,  C07C59/64 ,  C07C69/734 ,  C07D309/12 ,  C07F7/1856 ,  Y02P20/55

    摘要： Present invention relates to an improved and commercial process for the preparation of 2-sustituted-2-(6-(substituted)-7-methylbenzo[d][1,3]dioxol-4-yl)acetic acid derivatives of formula-I [Formula should be inserted here], wherein R 1 is a O-protecting group such as methoxymethyl, ethoxymethyl, trialkylsilyl, arylmethyl, tetrahydropyran-2-yl, allyl; X is hydroxyl, halogen, mesylate, triflate, tosylate, acetate; Y is oxygen atom, NH or sulfur atom; R 2 is C 1 -C 6 alkyl. 2,4-Dihydroxy-3-methylbenzaldehyde is selectively protected at C-4 position in the form of an ether compound of formula-XII, oxidized the aldehyde function to get the diol of formula-XIII, and condensed with ethyl glyoxalate under Casiraghi reaction conditions to get the compound of formula-XV. Compound of formula-XV is converted to compound of formula-I by conventional chemistry. Compounds of formula-I are key intermediates in the synthesis of ecteinascidines like trabectedin

    摘要翻译： 本发明涉及制备式I的2-取代-2-（6-（取代的）-7-甲基苯并[d] [1,3]二氧杂环戊烯-4-基）乙酸衍生物的改进和商业化方法 [在此应插入配方]，其中R 1是O-保护基，例如甲氧基甲基，乙氧基甲基，三烷基甲硅烷基，芳基甲基，四氢吡喃-2-基，烯丙基; X是羟基，卤素，甲磺酸酯，三氟甲磺酸酯，甲苯磺酸酯，乙酸酯; Y是氧原子，NH或硫原子; R2是C1-C6烷基。 2,4-二羟基-3-甲基苯甲醛在C-4位被选择性保护为式-IIII的醚化合物形式，氧化醛官能团以得到式-IIIIII的二醇，并在卡西拉希反应下与乙二醛酸乙酯缩合 得到式XV化合物的条件。 通过常规化学方法将式XV的化合物转化为式I的化合物。 式I的化合物是合成类似于trabectinin的ecteinascidine的关键中间体

    NOVEL CHALCONE DERIVATIVES WITH CYTOTOXIC ACTIVITY
    39.
    发明申请
    NOVEL CHALCONE DERIVATIVES WITH CYTOTOXIC ACTIVITY 审中-公开

    公开(公告)号：WO2011009826A3

    公开(公告)日：2011-01-27

    申请号：PCT/EP2010/060368

    申请日：2010-07-16

    申请人： ADAMED SP.Z O.O. ,  KONIECZNY, Marek ,  SKLADANOWSKI, Andrzej ,  LEMKE, Krzysztof ,  PIECZYKOLAN, Jerzy

    发明人： KONIECZNY, Marek ,  SKLADANOWSKI, Andrzej ,  LEMKE, Krzysztof ,  PIECZYKOLAN, Jerzy

    IPC分类号： C07C321/24 ,  C07D317/54 ,  C07D319/18 ,  C07D327/04 ,  C07D327/06 ,  A61K31/39 ,  A61P35/00 ,  C07D317/64

    摘要： Chalcone derivatives of the general formula (I), wherein two from among A, B and Z which are adjacent to each other are linked and form a moiety selected from -O-(CH 2 ) n -S(O) m -, -S(O) m -(CH 2 ) n -O- and -O-(CH 2 ) n -O-, and the remaining one from among A, B and Z is H; or two from among A, B and Z, independently from each other, are selected from a group consisting of OH, -O-C 1 -C 6 -alkyl and -S(O)m-C 1 -C 6 -alkyl, and the remaining one from among A, B and Z is H; R is H, C 1 -C 6 -alkyl, carboxy-C 1 -C 6 -alkyl, -(CH 2 ) P - NR 1 R 2 or O(CH 2 ) 3 NH(CO)CF 3 , where R 1 and R 2 both independently are C 1 -C 6 -alkyl; or R 1 and R 2 are linked together to form polymethylene group -(CH 2 ) q -, and with N atom, to which they are attached, form a 5- or 6-membered ring, in which one of carbon atoms may be optionally replaced with O, N, or S; Y is -CH=CH-, -O-, -S- or -CH=N-; X 1 , X 2 , X 3 independently are H, halogen atom, OH, -C 1 -C 6 -alkoxy, carboxy-C 1 -C 6 -alkoxyl, di(C 1 -C 6 - alkyl)amino-C 1 -C 6 -alkoxy, -0-PO(OH) 2 , NO 2 or NH 2 ; m = O, 1 or 2; n = 1 or 2; p = 2 to 6; q = 4 or 5; and acid addition salts, salts with bases and C 1 -C 6 -alkyl esters thereof. The compounds may be useful as cytotoxic drugs for the treatment of neoplastic diseases. Formula (I).