- Preparation method of 2-methyl-5-nitrophenyl guanidine
-
The invention relates to a preparation method of 2-methyl-5-nitrophenyl guanidine, and belongs to the technical field of synthesis of drug intermediates. In order to solve the problems of high reaction corrosivity and low yield in the prior art, the invention provides a preparation method of 2-methyl-5-nitrophenyl guanidine, which comprises the following step: in the presence of an acid-binding agent, carrying out a condensation reaction on 2-chloro-4-nitrotoluene and guanidine hydrochloride in an alcohol solvent to obtain the corresponding product 2-methyl-5-nitrophenyl guanidine. According to the method, high efficiency and conversion rate can be achieved, the product yield reaches 90% or above, and the purity reaches 99% or above. The reaction conditions are mild, the operation is easier, the cost is relatively low, and the industrial production is more facilitated.
- -
-
Paragraph 0041-0043
(2021/11/14)
-
- COMPOSITIONS AND METHODS FOR INHIBITING KINASES
-
The present invention provides methods for the prevention or treatment of Parkinson's Disease using Abelson-family tyrosine kinase inhibitors.
- -
-
Page/Page column 51; 52
(2018/05/24)
-
- COMPOSITIONS AND METHODS FOR INHIBITING KINASES
-
The present invention provides compounds for the prevention or treatment of cancer or a bacterial or viral infection. Additionally, the present invention provides compositions and methods for using these compounds and compositions in the prevention or treatment of cancer or a bacterial or viral infection in a subject.
- -
-
Page/Page column 33-34
(2016/11/14)
-
- Facile synthesis of 2-phenylquinoline-4-carboxamide derivatives with variant structural features
-
The quinoline scaffold is an important class of heterocyclic compounds that possesses diverse chemotherapeutic activities. Thus, the 2-phenylquinoline-4- carboxamide derivatives containing a variety of moieties, such as 2-(2-furanyl)-1,3,4-oxadiazole, N-(2-methylphenyl)-4-(3-pyridinyl)-2- pyrimidinamine, 4,4′-bithiazole, purine, adamantine and resorcinol, have been designed and synthesized via Suzuki coupling, acid-base coupling and other typical reactions.
- Islam, Rafiqul,Hossain, Md. Imran,Okamoto, Yoshinari,Nagamatsu, Tomohisa,Anraku, Kensaku,Okawara, Tadashi
-
p. 693 - 708
(2014/04/03)
-
- PROCESSES FOR THE PREPARATION OF IMATINIB BASE AND INTERMEDIATES THEREOF
-
The invention relates to an improved process for the preparation of highly pure imatinib base (99.99% HPLC purity) of formula (I) and the pharmaceutically acceptable acid addition salts thereof. This invention also relates to processes for the preparation of the intermediates in the synthesis of imatinib base.
- -
-
Page/Page column 21
(2013/03/26)
-
- A facile total synthesis for large-scale production of imatinib base
-
An efficient, economic process has been developed for the production of imatinib with 99.99% purity and 50% overall yield from four steps. Formation and control of all possible impurities is described. The synthesis comprises the condensation of N-(5-amino-2-methylphenyl)-4-(3-pyridinyl)-2-pyrimidineamine with 4-(4-methylpiperazinomethyl)benzoyl chloride in isopropyl alcohol solvent in the presence of potassium carbonate to yield imatinib base.
- Kompella, Amala,Adibhatla, Bhujanga Rao Kalisatya,Muddasani, Pulla Reddy,Rachakonda, Sreenivas,Gampa, Venugopala Krishna,Dubey, Pramod Kumar
-
p. 1794 - 1804
(2013/01/15)
-
- PROCESSES FOR PREPARING IMATINIB AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
-
The processes for preparing imatinib and its pharmaceutically acceptable salts, specifically imatinib mesylate, are disclosed.
- -
-
-
- PROCESS FOR THE PREPARATION OF IMATINIB AND INTERMEDIATES THEREOF
-
It is the object of the present invention a process for the preparation of 4-methyl-N3-[4-(3-pyridinyl)-2-pyrimidinyl]-1,3-benzenediamine and analogues thereof, intermediates useful for the synthesis of Imatinib, or 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide.
- -
-
Page/Page column 10
(2010/04/23)
-
- AMINOARYL SUBSTITUTED FIVE-MEMBERED RING HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF DISEASES
-
The present invention relates to novel compounds selected from aminoaryl five-membered ring heterocycles that selectively modulate, regulate and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a varie
- -
-
Page/Page column 35
(2010/11/08)
-
- 2-AMINOPYRIMIDINE DERIVATIVES AS RAF KINASE INHIBITORS
-
This application discloses compounds that inhibit Raf kinase having the formula (I), wherein R1 is a phenyl radical or a heteroaryl radical; and R2 is a phenyl radical; or an N-oxide or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of proliferative diseases, such as cancer.
- -
-
Page/Page column 24
(2010/02/09)
-
- Urea derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases
-
Urea-based analogues of STI571 are described possessing structural features which can differentiate between Abl/Bcr-Abl and PDGFR kinase inhibition. The constitutively active Abl kinase activity of the Bcr-Abl oncoprotein is causative for chronic myelogenous leukemia. Urea derivatives, structurally related to the therapeutic agent STI571, have been identified, which potently inhibit the tyrosine kinase activity of recombinant Abl. In particular a dimethylamino-aniline derivative (18) inhibited c-Abl transphosphorylation with an IC50 value of 56 nM. Although this activity was not translated into cellular activity against the constitutively activated oncogenic Bcr-Abl, a number of compounds from this series potently inhibited cellular PDGFR autophosphorylation. It was also possible to differentiate between c-Abl and PDGFR kinase inhibition, with compound 22 being selective towards Abl and 23 selective for PDGFR.
- Manley, Paul W.,Breitenstein, Werner,Brüggen, Josef,Cowan-Jacob, Sandra W.,Furet, Pascal,Mestan, Jürgen,Meyer, Thomas
-
p. 5793 - 5797
(2007/10/03)
-