9-isopropylidene-5-nitro-benzonorbornadiene 在
铑碳 、 氢气 作用下,
以
四氢呋喃 为溶剂,
反应 96.0h,
以to afford the title compound as an 87:13 syn的产率得到9-isopropyl-1,2,3,4-tetrahydro-1,4-methanonaphthalen-5-amine
Method for the Production of N-Substituted (3-Dihalomethyl-1-Methyl-Pyrazole-4-yl) Carboxamides
申请人:Zierke Thomas
公开号:US20100174094A1
公开(公告)日:2010-07-08
The present invention relates to a process for preparing N-substituted (3-dihalomethylpyrazol-4-yl)carboxamides of the formula (I)
in which R
1
is optionally substituted phenyl or C
3
-C
7
-cycloalkyl, R
1a
is hydrogen or fluorine, or R
1a
together with R
1
is optionally substituted C
3
-C
5
-alkanediyl or C
5
-C
7
-cycloalkanediyl, R
2
is C
1
-C
6
-alkyl, C
2
-C
6
-alkenyl, C
2
-C
6
-alkynyl or C
1
-C
4
-alkoxy-C
1
-C
2
-alkyl, X is F or Cl and n is 0, 1, 2 or 3; which comprises
A) providing a compound of the formula (II)
in which X is F or Cl, Y is Cl or Br and R
2
has one of the meanings given above and
B) reacting a compound of the formula (II) with carbon monoxide and a compound of the formula (III)
in which R
1
, R
1a
and n have one of the meanings given above; in the presence of a palladium catalyst;
to intermediates used for the preparation according to the process according to the invention, and also to processes for their preparation.
PRODUCTION METHOD FOR PYRAZOLE-4-CARBOXAMIDE DERIVATIVE
申请人:JAPAN FINECHEM COMPANY, INC.
公开号:US20200181091A1
公开(公告)日:2020-06-11
The present invention relates to a method of producing a pyrazole-4-carboxamide derivative including subjecting a pyrazole-4-carboxylic acid ester and an amine to an aminolysis reaction in a solvent in the presence of a base, provided that the reaction is completed without removing a by-produced alcohol or phenol outside the system. An industrial production method of a pyrazole-4-carboxamide derivative which is useful as an agricultural fungicide, simply and in high yield and high purity as compared with the conventional method, is provided.
A process for preparing arylcarboxamides of the formula (I)
where
Ar =a mono- to trisubstituted phenyl, pyridyl or pyrazolyl ring, where the substituents are selected from halogen, C
i
-C
4
-alkyl and C
1
-C
4
-haloalkyl;
M =thienyl or phenyl, which may bear a halogen substituent;
Q =direct bond, cyclopropylene, fused bicycio[2.2.1]heptane or bicyclo[2.2.1]heptene ring;
R
1
=hydrogen, halogen, C
1
-C
6
-alkyl, C
1
-C
4
-alkoxy, C
1
-C
4
-haloalkoxy, mono- to trisubstituted phenyl, where the substituents are selected from halogen and trifluoromethylthio, or cyclopropyl;
by reacting an acid chloride of the formula (II)
with an arylamine (III)
in a suitable nonaqueous solvent, wherein, in the absence of an auxiliary base,
a) the acid chloride (II) is initially charged,
b) a pressure of from 0 to 700 mbar is established,
c) the arylamine (III) is metered in in an approximately stoichiometric amount and
d) the product of value is isolated.
[EN] PROCESS FOR THE PREPARATION OF AMIDES<br/>[FR] PROCÉDÉ POUR LA FABRICATION D'AMIDES
申请人:SYNGENTA LTD
公开号:WO2009138375A1
公开(公告)日:2009-11-19
The invention relates to a process for the preparation of fungicidally active compounds such as tricyclic amine derivatives(I). The process involves coupling of a carboxylic 5 acid e.g. a compound of formula (II) with an aniline, e.g. a compound of formula(III) in the presence of a boronic acid catalystor an antimony catalyst (II)(III)(I) wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Het are defined in the specification.
[EN] PROCESS FOR THE PREPARATION OF PYRAZOLE-4-CARBOXAMIDES<br/>[FR] PROCÉDÉ DE PRÉPARATION DE PYRAZOLE-4-CARBOXAMIDES
申请人:SOLVAY
公开号:WO2012055864A1
公开(公告)日:2012-05-03
The invention concerns a process for the manufacture of pyrazole-4-carboxamides, in particular, of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxamides which are useful as pharmaceuticals and agrochemicals. The carboxamides are prepared from the corresponding pyrazole-4-carboxylic acid esters and appropriate amine in the presence of a base. The reaction is performed in a reaction medium which is essentially free of water; alternatively, the base is used in an amount equal to or greater than 0.25 equivalents per mole of amine.