公开(公告)号：WO2011154555A1

公开(公告)日：2011-12-15

申请号：PCT/EP2011/059823

申请日：2011-06-14

Applicant: SYNGENTA PARTICIPATIONS AG ,  SYNGENTA LIMITED ,  EL QACEMI, Myriem ,  SMITS, Helmars ,  CASSAYRE, Jérôme Yves ,  MULHOLLAND, Nicholas Phillip ,  RENOLD, Peter ,  GODINEAU, Edouard ,  PITTERNA, Thomas

Inventor： EL QACEMI, Myriem ,  SMITS, Helmars ,  CASSAYRE, Jérôme Yves ,  MULHOLLAND, Nicholas Phillip ,  RENOLD, Peter ,  GODINEAU, Edouard ,  PITTERNA, Thomas

IPC: C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  A01N43/80 ,  C07D207/20 ,  C07D401/04 ,  C07D403/04 ,  C07D409/12 ,  C07D409/14 ,  A01N43/36 ,  A01N43/40 ,  C07C1/32

CPC classification number: C07D207/46 ,  A01N43/36 ,  C07D207/20 ,  C07D401/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention provides stereoselective processes for the preparation of compounds of formula (I) wherein P is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted; R 1 is chlorodifluoromethyl or trifluoromethyl; R 2 is optionally substituted aryl or optionally substituted heteroaryl; n is 0 or 1; including the process comprising (a-i) reacting a compound of formula II wherein P, R 1 and R 2 are as defined for the compound of formula I; with nitromethane in the presence a chiral catalyst to give a compound of formula III Wherein P, R 1 and R 2 are as defined for the compound of formula I; and (a-ii) reductively cyclising the compound of formula III to give the compound of formula I. The invention also provides intermediates useful for processes for the synthesis of compounds of formula (I).

Abstract translation: 本发明提供了制备式（I）化合物的立体选择性方法，其中P是苯基，萘基，含有一个或两个氮原子作为环成员的6元杂芳基或含有一个或多个氮原子的10元双环杂芳基 两个氮原子作为环成员，并且其中苯基，萘基和杂芳基任选被取代; R1是氯二氟甲基或三氟甲基; R2是任选取代的芳基或任选取代的杂芳基; n为0或1; 包括（a-i）使式II化合物与式Ⅰ化合物反应的方法，其中P，R 1和R 2如对式I化合物所定义; 在硝基甲烷中存在手性催化剂，得到式III化合物，其中P，R 1和R 2如式I化合物所定义; 和（a-ii）还原性环化式III化合物以得到式I化合物。本发明还提供了可用于合成式（I）化合物的方法的中间体。

公开(公告)号：WO2011104089A1

公开(公告)日：2011-09-01

申请号：PCT/EP2011/051513

申请日：2011-02-03

Applicant: SYNGENTA PARTICIPATIONS AG ,  SYNGENTA LIMITED ,  MULHOLLAND, Nicholas Phillip ,  GODINEAU, Edouard ,  CASSAYRE, Jérôme Yves ,  RENOLD, Peter ,  EL QACEMI, Myriem ,  REVOL, Guillaume

Inventor： MULHOLLAND, Nicholas Phillip ,  GODINEAU, Edouard ,  CASSAYRE, Jérôme Yves ,  RENOLD, Peter ,  EL QACEMI, Myriem ,  REVOL, Guillaume

IPC: C07D413/12 ,  C07D413/14 ,  C07D453/04 ,  A01N43/82

CPC classification number: A01N43/80 ,  B01J31/0271 ,  C07D413/12 ,  C07D413/14 ,  C07D453/04

Abstract: The present invention relates to processes for the preparation of compounds of formula IB wherein A 1 , A 2 , A 3 , A 4 , L, Y 1 , Y 2 , R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the claims, comprising reacting a compound of formula (II) wherein Y 1 , Y 2 , L, A 1 , A 2 , R 1 , R 2 , R 3 , R 4 and R 5 are as defined for the compound of formula (I); with hydroxylamine in the presence of water, a base and a chiral phase transfer catalyst, which chiral phase transfer catalyst is a quinine derivative. The invention also relates to compounds of formula IB and enantiomerically enriched mixtures comprising compounds of formula IB.

Abstract translation: 本发明涉及制备式IB化合物的方法，其中A1，A2，A3，A4，L，Y1，Y2，R1，R2，R3，R4和R5如权利要求中所定义，包括使 式（II）其中Y1，Y2，L，A1，A2，R1，R2，R3，R4和R5如式（I）化合物所定义; 在水存在下用羟胺，碱和手性相转移催化剂，该手性相转移催化剂是奎宁衍生物。 本发明还涉及式IB化合物和包含式IB化合物的对映体富集的混合物。

公开(公告)号：WO2010130970A1

公开(公告)日：2010-11-18

申请号：PCT/GB2010/000892

申请日：2010-05-06

Applicant: SYNGENTA LIMITED ,  WILLETTS, Nigel, James ,  MULHOLLAND, Nicholas, Phillip ,  WORTHINGTON, Paul, Anthony ,  AVERY, Alaric, James

Inventor： WILLETTS, Nigel, James ,  MULHOLLAND, Nicholas, Phillip ,  WORTHINGTON, Paul, Anthony ,  AVERY, Alaric, James

IPC: C07D495/04 ,  A01N43/60

CPC classification number: C07D495/04 ,  A01N43/60 ,  C07D241/24

Abstract: The present invention relates to 6,6-dioxo-6-thia-1,4-diaza-naphthalene derivatives of formula (I) where R 1 , R 2 , R 3a , R 3b , R 4 and R 5 are as defined in claim 1; or a salt or N -oxide thereof. Furthermore, the present invention relates to processes and intermediates for making compounds of formula (I), to herbicidal compositions comprising compounds of formula (I) and to methods of using compounds of formula (I) to control plant growth.

Abstract translation: 本发明涉及式（I）的6,6-二氧代-6-硫杂-1,4-二氮杂萘衍生物，其中R1，R2，R3a，R3b，R4和R5如权利要求1所定义; 或其盐或N-氧化物。 此外，本发明涉及制备式（I）化合物的方法和中间体，包含式（I）化合物的除草组合物和使用式（I）化合物来控制植物生长的方法。