- Synthesis method of 6-fluoro-3-hydroxypyrazine-2-carboxylic acid
-
The invention belongs to medical intermediates, and particularly relates to a synthesis method of 6-fluoro-3-hydroxypyrazine-2-carboxylic acid. The 6-fluoro-3-hydroxypyrazine-2-carboxylic acid is prepared by taking a compound A, namely 3-aminopyrazine-2-carboxylic acid methyl ester as an initial raw material through five-step reaction, the synthetic method of the 6-fluoro-3-hydroxypyrazine-2-carboxylic acid is provided, a synthetic route is provided for the synthetic method of the 6-fluoro-3-hydroxypyrazine-2-carboxylic acid, the synthesis method of 6-fluoro-3-hydroxypyrazine-2-carboxylic acid provided by the invention is reasonable in design, simple to operate and easy to control, and meanwhile, the product obtained by the invention is relatively high in yield.
- -
-
Paragraph 0005; 0013-0015
(2021/07/21)
-
- Nitrogen-containing heterocyclic ring derivatives and preparation method and application thereof
-
The invention relates to nitrogen-containing heterocyclic ring derivatives. The nitrogen-containing heterocyclic ring derivatives have the following structures as described in the specification. In the structures, A, X, Y, Z, R1, R2a, R2b, R3a, R3b, R4a, R4b and m are as defined in the specification. The derivatives have good inhibition effect on protein tyrosine phosphatase SHP-2, and can be used for preparing antitumor drugs. The invention discloses a preparation method and application of the derivatives.
- -
-
Paragraph 0049-0052
(2021/06/26)
-
- Large-scale process for preparing 2-amino-3-bromo-6-chloropyrazine
-
The invention discloses a large-scale process for preparing 2-amino-3-bromo-6-chloropyrazine. The product is obtained from 3-aminopyrazine-2-carboxylate as a raw material through steps of chlorination, diazotization bromination, ester group hydrolysis, carboxyl rearrangement, t-butyloxycarbonyl removal and the like. The process is higher in yield, simple in purification, prone to large-scale production and capable of realizing effective and low-cost production.
- -
-
Paragraph 0032-0034
(2018/06/26)
-
- PYRIDO [2, 3-B] PYRAZINE DERIVATIVES USEFUL AS HERBICIDAL COMPOUNDS
-
The present invention relates to a method of controlling plants or inhibiting plant growth which comprises applying to the plants or to the locus thereof a herbicidally effective amount of a compound of formula (I) wherein R1, R2, R
- -
-
Page/Page column 64-65
(2008/06/13)
-
- Heterocyclic compounds
-
The invention concerns pharmaceutically useful compounds of the formula I, in which A1, A2, A3, A4, B1, m, Ar, W, X, Y, Z and R1 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.
- -
-
-
- N-heterocyclic sulfonamides having endothelin receptor activity
-
The invention concerns pharmaceutically useful compounds of the formula I, in which R 1, R 2, R 3, n, m and Het have any of the meanings defined herein, and their pharmaceutically-acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processess for the manufacture of the novel compounds and the use of the compounds in medical treatment.
- -
-
-