中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

9 records (took 0.01 seconds)

    Process of total synthesis of cephalosporin derivatives and intermediates
    1.
    发明授权
    Process of total synthesis of cephalosporin derivatives and intermediates 失效
    CEPHOROSPORIN衍生物和中间体的合成方法

    公开(公告)号：US3708477A

    公开(公告)日：1973-01-02

    申请号：US3708477D

    申请日：1970-10-16

    Applicant: ROUSSEL UCLAF

    Inventor： MARTEL J ,  HEYMES R

    IPC: A22B5/16 ,  C07D207/34 ,  C07D207/36 ,  C07D207/38 ,  C07D271/04 ,  C07D501/08 ,  C07D513/04 ,  F21V17/16 ,  G09F9/00 ,  H01H9/18 ,  H01H13/52 ,  C07D99/24

    CPC classification number: F21V17/16 ,  C07D207/34 ,  C07D207/36 ,  C07D207/38 ,  C07D271/04 ,  C07D501/08 ,  C07D501/18 ,  C07D501/38 ,  C07D501/42 ,  C07D501/46 ,  C07D513/04 ,  G09F9/00

    Abstract: PROCESS FOR THE PREPARATION OF RACEMIC OR OPTICALLYACTIVE CEPHALOSPORINE DERIVATIVES OF THE FORMULA

    2,3-(-CO-N(-R1)-CH2-),7-NH2-2-CEPHEM

    WHEREIN R1 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL, SUBSTITUTED AKYL, ARYL AND SUBSTITUTED ARYL, WHICH COMPRISES THE STEPS OF REACTING AN AMINO ACID OF THE FORMULA

    R1-NH-CH2-CH2-COOH

    WITH BENZYL ALCOHOL, CONDENSING THE BENZYL ESTER THUS OBTAINED WITH AN OXALATE, CONVERTING THE BENZYL ESTER OF 2,3DIOXI-4-CARBOXY-PYRROLIDINE INTO THE CORRESPONDING ACID, SUBJECTING SAID ACID TO AMINOMETHYLATION, THUS YIELDING A COMPOUND OF THE FORMULA

    1-R1,3-OH,4-(R"-N(-R'')-CH2-)PYRROL-3-IN-2-ONE

    CONVERTING SAID COMPOUND INTO THE CORRESPONDING 4-ACYLTHIOMETHYL DERIVATIVE, CONVERTING SAID DERIVATIVE INTO THE CORRESPONDING 4-THIOMETHYL DERIVATIVE, CONDENSING SAID DERIVATIVE WITH AN ENAMINE OF THE FORMULA

    R-OOC-C(-Y)=CH-NH2

    TO OBTAIN A THIAZINE DERIVATIVE OF THE FORMULA

    2-(Y-CH(-COO-R)-),5-R1-2,3,4,5,6,7-HEXAHYDRO-PYRROLO

    (3,4-D)-1,3-THIAZIN-4-ONE

    CONVERTING SAID THIAZINE DERIVATIVE INTO A COMPOUND OF THE FORMULA

    2-(H2N-CH(-COOH)-),5-R1-2,3,4,5,6,7-HEXAHYDRO-PYRROLO

    (3,4-)-1,3-THIAZIN-4-ONE

    SUBJECTING SAID COMPOUND TO THE ACTION OF A TRITYLATION AGENT, RECOVERING THE THREO ISOMER OF THE TRITYLATED DERIVATIVE, LACTAMIZING SAID THREO ISOMER TO OBTAIN THE Y-LACTAM OF DL-6H,7H-CIS-7-TRITYLAMINO-3-AMINOALKYL-CEPH 3-EME-4-CARBOXYLIC ACID, DETRITYLATING SAID Y-LACTAM AND RECOVERING SAID RACEMIC OF OPTICALLY ACTIVE CEPHALOSPORIN DERIVATIVES. THESE COMPOUNDS ARE USEFUL AS INTERMEDIATES IN THE PREPARATION OF THE CORRESPONDING 7ACYLAMINO DERIVATIVES OF THE FORMULA

    2,3-(-CO-N(-R1)-CH2-),7-(R2-NH-)-2-CEPHEM

    WHEREIN R1 HAS THE ABOVE DEFINITION AND R2 IS THE ACYL OF AN ORGANIC CARBOXYLIC ACID WHICH COMPOUNDS ARE ALSO PART OF THE INVENTION AND ARE USEFUL AS ANTIBIOTICS.

    Novel cyclopropanecarboxylic acids
    2.
    发明授权
    Novel cyclopropanecarboxylic acids 失效
    新型环糊精羧基酸

    公开(公告)号：US3714153A

    公开(公告)日：1973-01-30

    申请号：US3714153D

    申请日：1970-06-22

    Applicant: ROUSSEL UCLAF

    Inventor： MARTEL J ,  BUENDIA J

    IPC: A01N53/04 ,  A01N53/10 ,  C07D207/38 ,  C07D307/45 ,  C07D307/54 ,  C07D307/58 ,  C07D333/32 ,  C09B23/00

    CPC classification number: C07D307/42 ,  C07D207/38 ,  C07D307/54 ,  C07D307/58 ,  C07D333/32

    Abstract: Novel 3,3-dimethyl-2-(2''-oxo-3''-x-cyclopentylidenemethyl)-1cyclopropanecarboxylic acids of a cis or trans structure, in the form of racemic mixtures or optically active isomers of the formula

    WHEREIN X is selected from the group consisting of oxygen, sulfur and imino and R is selected from the group consisting of hydrogen, lower alkyl of one to six carbons, a radical of the formula

    WHEREIN Y3 is aryl such as phenyl, and a radical of the formula

    WHEREIN Z is alkenyl or alkadienyl such as allyl, butenyl and pentadienyl and their preparation and intermediates therefor.

    Abstract translation: 具有下式的外消旋混合物或光学活性异构体的顺式或反式结构的新的3,3-二甲基-2-（2'-氧代-3'-x-环戊基亚甲基）-1-环丙烷甲酸为式WHEREIN X 选自氧，硫和亚氨基，R选自氢，1至6个碳的低级烷基，式WHEREIN Y 3为芳基如苯基的基团和式 其中Z是烯基或链二烯基，例如烯丙基，丁烯基和戊二烯基及其制备方法和中间体。

    Aryl allyl sulfones
    3.
    发明授权
    Aryl allyl sulfones 失效
    ARYL ALLYL SULFONES

    公开(公告)号：US3711555A

    公开(公告)日：1973-01-16

    申请号：US88563469

    申请日：1969-12-16

    Applicant: ROUSSEL UCLAF

    Inventor： MARTEL J ,  HUYNH C

    IPC: C07C21/14 ,  C07C22/04 ,  C07C35/04 ,  C07C317/14 ,  C07D307/45 ,  C07D307/54 ,  C07D309/04 ,  C07D309/10 ,  C07D309/20 ,  C07C147/06

    CPC classification number: C07D307/42 ,  C07C21/14 ,  C07C22/04 ,  C07C35/045 ,  C07C317/00 ,  C07D307/54 ,  C07D309/04 ,  C07D309/10 ,  C07D309/20

    Abstract: Aryl allyl sulfones of the formula WHEREIN Ar is phenyl optionally substituted with lower alkyl, lower alkoxy, halomethyl, nitro or halogen and HA has the formula WHEREIN R''1 is hydrogen or lower alkyl and FORM FLUORENE OR SATURATED OR UNSATURATED CYCLOALKYL OF THREE TO SEVEN CARBON ATOMS OPTIONALLY SUBSTITUTED WITH ONE OR MORE LOWER ALKYL AND/OR LOWER ALKOXY USEFUL AS INTERMEDIATES IN THE PREPARATION OF CYCLOPROPANECARBOXYLIC ACID ESTERS HAVING INSECTICIDAL ACTIVITY.

    Abstract translation: 式WHEREIN Ar的芳基烯丙基砜是任选被低级烷基，低级烷氧基，卤代甲基，硝基或卤素取代的苯基，HA具有式WHEREIN R'1是氢或低级烷基，并且三氟甲磺酸或饱和或不饱和环烷基三 选择性地采用一种或多种较低的碱性和/或较低的碱性的碳原子作为具有杀虫活性的环糊精羧酸酯的制备中的中间体。

    Cyclopentanone derivatives
    5.
    发明授权
    Cyclopentanone derivatives 失效
    环戊烷酮衍生物

    公开(公告)号：US3801623A

    公开(公告)日：1974-04-02

    申请号：US3801623D

    申请日：1971-04-28

    Applicant: ROUSSEL UCLAF

    Inventor： MARTEL J ,  TOROMANOFF E ,  BUENDIA J

    IPC: C07C59/90 ,  C07C405/00 ,  C07D309/12 ,  C07C69/36 ,  C07C69/74

    CPC classification number: C07C405/00 ,  C07C59/90 ,  C07D309/12

    Abstract: NOVEL PROSTANOIC ACID DERIVATIVES OF THE FORMULA

    2-R1,2-(R-OOC-(CH2)N-CH=CH-CH2-),3-(CH3-(CH2)M-CH(-O-R3)-

    CH=CH-),5-R2-CYCLOPENTANONE

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

    Process for the preparation of cyclopropane derivatives and compounds produced therein
    6.
    发明授权
    Process for the preparation of cyclopropane derivatives and compounds produced therein 失效
    制备环丙基衍生物的方法及其生产的化合物

    公开(公告)号：US3723469A

    公开(公告)日：1973-03-27

    申请号：US3723469D

    申请日：1969-07-11

    Applicant: ROUSSEL UCLAF

    Inventor： MARTEL J

    IPC: A01N53/00 ,  A47F5/00 ,  A47K1/09 ,  C07C51/00 ,  C07C61/35 ,  C07C61/37 ,  C07D307/93 ,  C07D5/34

    CPC classification number: C07D307/93 ,  A01N53/00 ,  A47F5/00 ,  C07C51/00 ,  C07C61/35 ,  C07C61/37

    Abstract: WHEREIN THE CO2H substituent on the carbon 1 and the

    Process for the preparation of an internal hemiacylal of racemic or optically active cis 3,3-dimethyl-2-formyl-cyclopropane-1carboxylic acid which are intermediates for the preparation of racemic or optically-active cyclopropane carboxylic acid of the formula
    SUBSTITUENT ON THE CARBON 2 ARE IN THE CIS-POSITION RELATIVE TO ONE ANOTHER, R1 represents a hydrogen, an alkyl radical, an aralkyl radical, an aryl radical, an alkenyl radical, an alkynyl radical, a cycloalkyl radical, a cycloalkenyl radical, a heterocyclic radical, these radicals being able to be substituted, specifically by lower alkyl or lower alkoxy, or represents a cyano group, an acyl group, a formyl group, an alkoxy-carbonyl group or a nitro group, and Z represents the R2 residue which has the same meaning as R1 but is identical or different thereto, or the R3 residue, which represents an allyl radical, a benzyl radical, a cyano group, an acyl group, a formyl group, an alkoxycarbonyl group, or a nitro group, or R1 and Z together form a saturated or unsaturated carbon homocycle or heterocycle, whose ring can support substituents such as lower alkyls or lower alkoxys, or functions such as ketonic functions, or together form a polycyclic aromatic residue such as a fluorene residue.

    Abstract translation: 用于制备外消旋或光学活性的顺式3,3-二甲基-2-甲酰基 - 环丙烷-1-羧酸的内部半胱氨酸的方法，其是用于制备下式的外消旋或光学活性环丙烷羧酸的中间体： 碳原子上的CO 2 H取代基和碳2上的取代基相对于另一个在CIS中的位置，R1表示氢，烷基，芳烷基，芳基，烯基，炔基， 环烷基，环烯基，杂环基，这些基团能够被低级烷基或低级烷氧基取代，或表示氰基，酰基，甲酰基，烷氧基 - 羰基或硝基 Z表示与R 1相同或相同或不同的R 2残基，或表示烯丙基，苄基，氰基，酰基，甲酰基， 烷氧基羰基或硝基，或者R 1和Z一起形成饱和或不饱和的碳均碳环或杂环，其环可以支持取代基如低级烷基或低级烷氧基，或诸如酮功能的功能，或一起形成多环芳族残基 如芴残留物。

    Process and intermediates in the preparation of eburnamonine
    9.
    发明授权
    Process and intermediates in the preparation of eburnamonine 失效
    制备EBURNAMONINE的过程和中间体

    公开(公告)号：US3753995A

    公开(公告)日：1973-08-21

    申请号：US3753995D

    申请日：1971-12-28

    Applicant: ROUSSEL UCLAF

    Inventor： MARTEL J ,  COSTEROUSSE G

    IPC: C07D461/00 ,  C07D471/14 ,  C07D57/08

    CPC classification number: C07D471/14 ,  C07D461/00

    Abstract: THE OBJECT OF THIS INVENTION IS A NEW PROCESS OF PREPARATION OF ($) EBURNAMONINE OF THE FORMULA:

    12-(O=),13A-(CH3-CH2-)-2,3,4A,5,6,12,13,13A-OCTAHYDRO-

    1H-INDOLO(3,2,1-DE)PYRIDO(3,2,1-IJ)(1,5)NAPHTHYRIDINE

    IT IS KNOWN THAT EBURANAMONINE HAS BEEN ISOLATED FROM SEVERAL PLANT SPECIES SUCH AS VINCA MINOR AND HUNTERIA EBURNEA. EBURNAMONINE POSSESSES INTERESTING PHARMACOLOGICAL PROPERIES, IT PROVOKES A HYPERTENSION ACCOMPANIED BY A RESPIRATORY AND CARDIAC STIMULATION AND AN INCREASE OF TONICITY. IN ADDITION, EBURNAMONINE CAN SERVE AS STARTING MATERIAL IN THE SYNTHESIS OF KNOWN ANALOGOUS COMPOUNDS DISPLAYING AN INTERESTING PHYSIOLOGICAL ACTIVITY.

Patent Agency Ranking