公开(公告)号：WO1995000480A1

公开(公告)日：1995-01-05

申请号：PCT/US1994005982

申请日：1994-05-26

Applicant: MERRELL DOW PHARMACEUTICALS INC.

Inventor： MERRELL DOW PHARMACEUTICALS INC. ,  KRAUSS, Richard, C. ,  STROM, Robert, M. ,  SCORTICHINI, Carey, L. ,  KRUPER, William, J. ,  WOLF, Richard, A. ,  CARR, Albert, A. ,  RUDISILL, Duane, E. ,  PANZONE, Gianbattista ,  HAY, David, A. ,  WU, Weishi, W.

IPC: C07D211/14

CPC classification number: C07D295/185 ,  C07C33/46 ,  C07C45/46 ,  C07C45/63 ,  C07C45/65 ,  C07C45/673 ,  C07C49/792 ,  C07C49/798 ,  C07C49/80 ,  C07C49/813 ,  C07C49/82 ,  C07C49/825 ,  C07C49/83 ,  C07C49/835 ,  C07C49/86 ,  C07C59/86 ,  C07C59/88 ,  C07C69/007 ,  C07C69/738 ,  C07C235/78 ,  C07C255/16 ,  C07C259/06 ,  C07C2601/02 ,  C07D211/22 ,  C07D401/06 ,  C07D401/10

Abstract: The present invention is related to novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of formula (I) wherein W represents -C(=O)- or -CH(OH)-; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is -COOH or -COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.

Abstract translation: 本发明涉及可用于制备其中W表示-C（= O） - 或-CH（OH） - 的式（I）的某些抗组氨酸哌啶衍生物的新型中间体和方法; R1代表氢或羟基; R2表示氢; R1和R2一起形成带有R1和R2的碳原子之间的第二个键; n为1〜5的整数， m为整数0或1; R3是-COOH或-COO烷基，其中烷基部分具有1至6个碳原子并且是直链或支链的; A中的每一个是氢或羟基; 和其药学上可接受的盐和单独的光学异构体，条件是其中R 1和R 2一起形成在具有R 1和R 2的碳原子之间或其中R 1表示羟基的第二个键，m是整数0。

公开(公告)号：WO1993020035A1

公开(公告)日：1993-10-14

申请号：PCT/JP1993000414

申请日：1993-04-01

Applicant: NIPPON SODA CO., LTD. ,  INOUE, Tsutomu ,  TAKATA, Mitsumasa ,  SUZUKI, Tatsumi ,  SAITO, Kenji ,  ISHIMITSU, Keiichi

Inventor： NIPPON SODA CO., LTD.

IPC: C07C49/433

CPC classification number: C07C323/62 ,  C07C49/433 ,  C07C49/657 ,  C07C49/792 ,  C07C62/24 ,  C07C69/757 ,  C07C317/24 ,  C07C317/46

Abstract: A process for producing a compound represented by general formula[I] according to scheme (A), wherein R represents alkyl; R represents alkyl, optionally substituted phenyl, optionally substituted aralkyl or optionally substituted heterocycle; R and R represent each alkyl; X and X represent each halogen; L represents a leaving group; and M represents a metal atom.

Abstract translation: 根据方案（A）制备由通式[I]表示的化合物的方法，其中R 1表示烷基; R 2表示烷基，任选取代的苯基，任选取代的芳烷基或任选取代的杂环; R 3和R 4各自表示烷基; X 1和X 2代表每个卤素; L表示离去基团; M表示金属原子。

公开(公告)号：WO1991001289A1

公开(公告)日：1991-02-07

申请号：PCT/JP1990000896

申请日：1990-07-12

Applicant: NIPPON SODA CO., LTD. ,  UEDA, Akiyoshi ,  SUGA, Shigemi ,  MIYAZAWA, Yasuyuki ,  AIHARA, Toshio ,  TOMIDA, Kazuyuki ,  YAMAGISHI, Hideki ,  HOSAKA, Hideo

Inventor： NIPPON SODA CO., LTD.

IPC: C07C49/713

CPC classification number: C07C49/84 ,  A01N35/06 ,  A01N35/10 ,  A01N41/10 ,  C07C49/417 ,  C07C49/517 ,  C07C49/657 ,  C07C49/683 ,  C07C49/693 ,  C07C49/697 ,  C07C49/723 ,  C07C49/743 ,  C07C49/747 ,  C07C49/753 ,  C07C49/792 ,  C07C49/798 ,  C07C49/835

Abstract: Substituted cyclohexanedione derivatives of general formula (I), and their salts, enamine and analogous derivatives, acylates, sulfonates, carbamates, and ether derivatives, each having herbicidal and plant growth regulating actions, wherein R represents lower alkyl or optionally substituted phenyl, aralkyl or heterocyclic group; Y represents straight-chain or branched lower alkylene; m is 0 or 1; R represents hydrogen or straight-chain or branched lower alkyl; R groups may be the same or different from one another and each represents halogen, cyano, alkyl, haloalkyl, cyanoalkyl, alkoxycarbonyl, or optionally substituted phenyl; n is 0, 1, 2, 3, 4 or 5; Z represents W or OR ; Z represents SR or OR , or alternatively Z and Z are combined together to represent oxygen, CR R or N-r, wherein R represents hydrogen or alkyl, R represents hydrogen, alkyl, alkenyl, alkoxyalkyl, alkylthioalkyl, or optionally substituted phenyl, and r represents hydrogen, alkyl, alkoxy, haloalkoxy, alkenyloxy, or haloalkenyloxy; W represents halogen, SR or OR ; R represents optionally substituted phenyl or heterocyclic group; R and R each represents alkyl or optionally substituted phenyl or heterocyclic group; and R represents alkyl or two R groups are combined together to represent alkylene.

Abstract translation: 通式（I）的取代的环己二酮衍生物及其盐，烯胺和类似衍生物，酰化物，磺酸盐，氨基甲酸盐和醚衍生物，各自具有除草和植物生长调节作用，其中R 1表示低级烷基或任选取代的苯基 ，芳烷基或杂环基; Y表示直链或支链低级亚烷基; m为0或1; R 2表示氢或直链或支链的低级烷基; R 3基团可以彼此相同或不同，并且各自表示卤素，氰基，烷基，卤代烷基，氰基烷基，烷氧基羰基或任选取代的苯基; n为0，1，2，3，4或5; Z 1表示W或OR 9; Z 2表示SR 6或OR 9，或者Z 1和Z 2组合在一起代表氧，CR 4 R 5或Nr，其中R 4表示 氢或烷基，R 5表示氢，烷基，烯基，烷氧基烷基，烷硫基烷基或任选取代的苯基，r表示氢，烷基，烷氧基，卤代烷氧基，烯氧基或卤代烯氧基。 W表示卤素，SR 7或OR 8; R 6表示任选取代的苯基或杂环基; R 7和R 8各自表示烷基或任选取代的苯基或杂环基; R 9代表烷基或两个R 9基团组合在一起代表亚烷基。

公开(公告)号：WO1991000260A1

公开(公告)日：1991-01-10

申请号：PCT/JP1990000850

申请日：1990-06-29

Applicant: NIPPON SODA CO., LTD. ,  UEDA, Akiyoshi ,  SUGA, Shigemi ,  ADACHI, Hiroyuki ,  AIHARA, Toshio ,  TOMIDA, Kazuyuki ,  YAMAGISHI, Hideki ,  HOSAKA, Hideo

Inventor： NIPPON SODA CO., LTD.

IPC: C07C205/45

CPC classification number: C07D213/70 ,  A01N35/06 ,  A01N37/18 ,  A01N37/42 ,  A01N41/06 ,  A01N41/10 ,  A01N43/40 ,  A01N43/56 ,  A01N43/78 ,  C07C45/673 ,  C07C45/676 ,  C07C49/433 ,  C07C49/477 ,  C07C49/517 ,  C07C49/733 ,  C07C49/747 ,  C07C49/792 ,  C07C49/813 ,  C07C49/84 ,  C07C65/36 ,  C07C69/76 ,  C07C205/45 ,  C07C255/56 ,  C07C317/24 ,  C07C2602/20 ,  C07D213/50 ,  C07D213/61 ,  C07D231/16 ,  C07D277/34

Abstract: This invention relates to substituted bicycloheptandione derivatives with high herbicidal activity which are represented by general formula (I), where R1 is a lower alkyl group, a phenyl group which may be substituted, an aralkyl group which may be substituted, or a heterocyclic group which may be substituted; R2 is, same or different, a halogen, an alkoxy group, an alkylthio group, an alkylsulfonyl group, an alkyl group, an alkoxyalkyl group, or an alkoxylcarbonyl group, and n is 0 to 4; R?3 and R4¿ are same or different, hydrogen or a lower alkyl group.

公开(公告)号：WO1989003812A1

公开(公告)日：1989-05-05

申请号：PCT/EP1988000901

申请日：1988-10-08

Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER ...

Inventor： MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER ... ,  POETSCH, Eike ,  MEYER, Volker ,  BÖTTCHER, Henning

IPC: C07B37/00

CPC classification number: C07D213/64 ,  C07C1/325 ,  C07C17/263 ,  C07C43/205 ,  C07C49/792 ,  C07C49/813 ,  C07C255/50 ,  C07C2601/14 ,  C07D213/26 ,  C07D213/80 ,  C07D237/08 ,  C07D237/14 ,  C09K19/40 ,  C07C13/28 ,  C07C25/18

Abstract: Compounds of formula (I): R1-(Ao)k-(Z1-A1)m-Zo-(E)n-(Q)o-(Z2-A2)p-R2 can be produced easily and in large quantities by transition metal catalysis from organotitanium compounds of formula (II): R1-(Ao)-(Z1-A1)m-Zo-Ti(Y)3 and compounds of formula (III): X-(E)n-(Q)o-(Z2-A2)p-R2, where Ao, A1, A2, E, R1, R2, Zo, Z1, Z2, Q, X, Y, k, m, n, o and p in formulae (I), (II) and (III) have the meaning given in the description.

公开(公告)号：WO8802357A3

公开(公告)日：1988-06-16

申请号：PCT/EP8700527

申请日：1987-09-16

Applicant: MERCK PATENT GMBH

Inventor： POETSCH EIKE ,  REIFFENRATH VOLKER

IPC: B01J31/16 ,  B01J31/24 ,  C07B31/00 ,  C07B37/00 ,  C07B37/04 ,  C07B61/00 ,  C07C1/00 ,  C07C1/32 ,  C07C13/28 ,  C07C15/54 ,  C07C17/00 ,  C07C17/26 ,  C07C17/263 ,  C07C23/18 ,  C07C25/18 ,  C07C41/00 ,  C07C43/21 ,  C07C43/225 ,  C07C45/00 ,  C07C49/76 ,  C07C49/782 ,  C07C49/792 ,  C07C49/813 ,  C07C67/00 ,  C07C253/00 ,  C07C255/50 ,  C07C325/00 ,  C07D239/26 ,  C07F3/06 ,  C09K19/04 ,  C09K19/30 ,  C09K19/34 ,  C07B41/00 ,  C07B43/00

CPC classification number: C07C255/00 ,  C07C13/28 ,  C07C15/54 ,  C07C25/18 ,  C07C43/21 ,  C07C49/792 ,  C07C49/813 ,  C07D239/26 ,  C09K19/3001

Abstract: Compounds having formula (I): R1-(Ao)k-(Z1-A1)m-Zo-(E)n-(Q)o-(Z2-A2)p-R2, can be easily produced in high yields from organic zinc compounds having formula (II): R1-(Ao)k-(Z1-A1)m-Zo-ZnY and compounds having formula (III): X-(E)n-(Q)o-(Z2-A2)p-R2, in which Ao, A1, A2, E, R1, R2, Zo, Z1, Z2, Q, k, m, n, o and p have the given meaning.