公开(公告)号：US20100056820A1

公开(公告)日：2010-03-04

申请号：US12522211

申请日：2008-01-21

Applicant: Volker Maywald ,  Christian Ott ,  Bernd Wolf ,  Manfred Ehresmann ,  Michael Rack ,  Michael Keil ,  Sebastian Peer Smidt

Inventor： Volker Maywald ,  Christian Ott ,  Bernd Wolf ,  Manfred Ehresmann ,  Michael Rack ,  Michael Keil ,  Sebastian Peer Smidt

IPC: C07C69/34

CPC classification number: C07C17/12 ,  C07C67/343 ,  C07C25/13 ,  C07C69/65

Abstract: The present invention relates to a process for preparing substituted 2-arylmalonic esters of the general formula I in which R is C1-C6-alkyl or C1-C4-alkoxy-C1-C4-alkyl; Ar is phenyl or a heteroaromatic 5- or 6-membered ring; where each carbon atom present in the radicals mentioned above optionally carries a substituent RA; RA is F, Cl, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, etc., or two adjacent substituents RA together with the carbon atoms to which they are attached form a ring; and where a malonic ester is reacted with a base and an aryl bromide in the presence of a copper salt, which comprises employing from 0.1 to 0.65 molar equivalents of the base per molar equivalent of the malonic ester.

Abstract translation: 本发明涉及制备通式Ⅰ的取代的2-芳基丙二酸酯的方法，其中R是C 1 -C 6 - 烷基或C 1 -C 4 - 烷氧基-C 1 -C 4烷基; Ar是苯基或杂芳族5或6元环; 其中存在于上述基团中的每个碳原子任选地带有取代基RA; RA是F，Cl，CN，NO 2，C 1 -C 4 - 烷基，C 1 -C 4卤代烷基，C 1 -C 4 - 烷氧基，C 1 -C 4 - 卤代烷氧基等，或两个相邻的取代基RA与它们 连接形成环; 并且其中丙二酸酯在铜盐存在下与碱和芳基溴反应，其包括使用每摩尔当量丙二酸酯0.1至0.65摩尔当量的碱。

公开(公告)号：US20100087640A1

公开(公告)日：2010-04-08

申请号：US12521877

申请日：2008-01-10

Applicant: Bernd Wolf ,  Volker Maywald ,  Michael Keil ,  Manuel Budich ,  Michael Rack ,  Manfred Ehresmann

Inventor： Bernd Wolf ,  Volker Maywald ,  Michael Keil ,  Manuel Budich ,  Michael Rack ,  Manfred Ehresmann

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates to a process for preparing aryl-substituted fused pyrimidines of the general formula (I) in which L1 to L5 are H, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy etc.; Y1 to Y3 are C—RY or N; RY is H or optionally substituted C1-C4-alkyl or two adjacent RY together form a ring; X is OH, Cl or Br; which comprises (i) the reaction of a 2-phenylmalonate with a compound (III) or a tautomer thereof, in the presence of a suitable base, where the alcohol, released during the reaction, of the formula R—OH is continuously removed from the reaction mixture under reduced pressure; giving a compound of the formula (I) or a salt thereof in which X is OH, and, if X in the compounds of the general formula (I) is chlorine or bromine, (ii) the reaction of the compounds of the formula (I) obtained in step (i) or the salts with a halogenating agent.

Abstract translation: 本发明涉及制备通式（I）的芳基取代的稠合嘧啶的方法，其中L 1至L 5为H，卤素，CN，NO 2，C 1 -C 4烷基，C 1 -C 4卤代烷基，C 1 -C 4 - 烷氧基，C1-C4-卤代烷氧基等; Y1至Y3为C-RY或N; RY为H或任选取代的C 1 -C 4烷基或两个相邻的RY一起形成环; X是OH，Cl或Br; 其包括（i）2-苯基丙二酸酯与化合物（III）或其互变异构体在合适的碱的存在下反应，其中反应期间释放的醇与式R-OH的连续从 减压下的反应混合物; 得到其中X是OH的式（I）化合物或其盐，并且如果通式（I）的化合物中的X是氯或溴，则（ii）式（I）化合物 I）或与卤化剂的盐。

公开(公告)号：US07314948B2

公开(公告)日：2008-01-01

申请号：US10485209

申请日：2002-08-02

Applicant: Steffen Kudis ,  Rene Lochtman ,  Manfred Ehresmann ,  Michael Keil ,  Joachim Gebhardt ,  Michael Rack ,  Ralf Schimetzek

Inventor： Steffen Kudis ,  Rene Lochtman ,  Manfred Ehresmann ,  Michael Keil ,  Joachim Gebhardt ,  Michael Rack ,  Ralf Schimetzek

IPC: C07C23/02

CPC classification number: C07C201/04 ,  C07C203/00

Abstract: In a continuous process for the preparation of alkyl nitrites and dinitrites, an alkanol or dialkanol is first mixed with an aqueous mineral acid, the reaction mixture obtained is then reacted with an inorganic nitrite and the product obtained can then be isolated immediately.

Abstract translation: 在制备亚硝酸烷基酯和二硝酸烷基酯的连续方法中，首先将烷醇或二烷醇与无机酸水溶液混合，然后将得到的反应混合物与无机亚硝酸盐反应，然后立即分离得到的产物。