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N-phenyl-2-pyrimidine-amine derivatives and process for the preparation thereof
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A pyrimidine and phenyl technology, applied in the field of N-phenyl-2-pyrimidine-amine derivatives and their salts, can solve the problems of toxic gas, no curative effect, explosion, etc.
Active Publication Date: 2008-04-02
IL YANG PHARMA CO LTD
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And, unlike other anticancer drugs, the compound is only effective in CML and has little effect on other parts of the body
Its synthesis sequence is that 4-chloromethylbenzoic acid 4-chloromethylbenzoic acid is first combined with N-methylpiperazine, then chlorinated with thionylchloride, and the resulting side group is combined with the basic structure, wherein chlorine The use of sulfoxide can cause many problems such as generation of toxic gas, explosion, reduction of reaction yield, etc.
In particular, the stability of intermediates adversely affects the overall yield of the compound
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preparation example 1
[0064] Preparation of 3-Dimethylamino-1-thiazol-2-yl-propenone
[0065] 2-Acetythiazole (35g, 0.275mol) and N,N-dimethylformyl dimethyl acetal (55ml, 0.412mol) were added to the reactor at room temperature (RT), then heated and heated at 70~ Mix at 80°C for 4 hrs. The mixture was cooled to room temperature, 30 mL of ether was added, and mixed in an ice bath for 1 hr. The resulting orange solid was filtered and dried at room temperature to afford the title compound as a yellow solid.
[0068] Preparation of 3-Dimethylamino-1-pyrazin-2-yl-propenone
[0069] Following the steps similar to Preparation 1, substituting 2-acetylpyrazine for 2-acetylthiazole, the title compound was obtained as a yellow solid.
[0072] Preparation of 3-Dimethylamino-1-(3-methylpyrazin-2-yl)-propenone
[0073] Following the similar steps of Preparation 1, substituting 2-acetyl-3-methylpyrazine for 2-acetylthiazole, the title compound was obtained as a brown solid.
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Abstract
The present invention relates to a novel N-phenyl-2-pyrimidine-amine derivative represented by the above formula (1) and its salt showing a superior effect on cancer in warm-blooded animals, such as lungcancer, gastric cancer, colon cancer, pancreatic cancer, hepatoma, prostatic cancer, breast cancer, chronic or acute leukemia, hematologic malignancy, encephalophyma, bladder cancer, rectal cancer, cervical cancer, lymphoma, etc. The present invention also relates to a process for preparing the compound, and to a pharmaceutical composition for the treatment of the above various diseases, which comprises an effective amount of the compound as an active ingredient together with pharmaceutically acceptable inert carriers.
Description
technical field [0001] The present invention relates to a kind of N-phenyl-2-pyrimidine-amine derivative and its salt represented by formula (1), [0002] [0003] in [0004] R 1 represents optionally substituted thiazole, imidazole, pyrazine or pyridine (wherein the substituent is amino or lower alkyl); [0005] R 2 , R 3 and R 6 independently represent hydrogen, halogen, lower alkyl or lower alkoxy; [0006] R 4 and R 5 each independently represents hydrogen, halogen, lower alkyl or lower alkoxy; or [0007] R 4 or R 5 independently represent groups shown in the following formula (2): [0008] [0009] where R 7 Represents lower alkyl or lower alkyl substituted with 1 to 3 halogens, [0010] R 8 represents an aliphatic group having 5 to 10 carbon atoms, or represents a saturated or unsaturated monocyclic group of 5 to 7 atoms, or a bi- or tri-cyclic group optionally combined with a benzene ring, each The benzene rings all contain 1 to 3 heteroatoms sele...
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