- A Palumbo vial preparation method of the key intermediate (by machine translation)
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The invention discloses a Palumbo Xilin key intermediate 6 - bromo - 2 - methyl sulfonyl - 8 - cyclopentyl - 5 - methyl pyridine and (2, 3 - d) pyrimidine - 7 (8 H) - ketone. The method uses the thiourea pyrimidine as the starting material, by methylation, chloro, bromo synthesis of 5 - bromo - 4 - chloro - 2 - methylthio-pyrimidine, then with the cyclopentamine alkylation, with 2 - butenoic acid by the heck reaction, then the intramolecular acylation reaction for the synthesis of 2 - methylthio - 8 - cyclopentyl - 5 - methyl pyridine and (2, 3 - d) pyrimidine - 7 (8 H) - one, finally with the NBS reaction for the preparation of 6 - bromo - 2 - methyl sulfonyl - 8 - cyclopentyl - 5 - methyl pyridine and (2, 3 - d) pyrimidine - 7 (8 H) - one. The preparation process of the present invention short step, not using the dangerous process, simple and convenient operation, low cost of raw materials, to meet the using requirements of the people. (by machine translation)
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Paragraph 0008; 0010
(2018/03/24)
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- SUBSTITUTED PYRIMIDINES
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The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
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Page/Page column 54-55
(2011/11/06)
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- SUBSTITUTED PYRIMIDINES
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The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
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Page/Page column 53-54
(2011/11/06)
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- CYCLIC COMPOUNDS
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There is provided a CRF receptor antagonist comprising a compound of the formula (I): A-W-Ar wherein, A is a group represented by the formula (A1) or (A2) (wherein, ring Aa is a 5-or 6-membered ring which may be further substituted; ring Ab is a 5-or 6-membered ring which may be further substituted; ring Ac is a 5- or 6-membered ring which may be substituted; R1 is optionally substituted alkyl, substituted amino, substituted hydroxy, etc.; X is carbonyl, -O-, -S-, etc.; Y1, Y2 and Q are independently optionally substituted carbon or nitrogen; … is a single or double bond); W is a bond, optionally substituted methylene, optionally substituted imino, -O-, -S-, etc.; Ar is optionally substituted aryl or optionally substituted heteroaryl; or a salt thereof or a prodrug thereof.
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Page/Page column 173
(2010/02/14)
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- Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
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The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
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Page/Page column 117-118
(2010/01/31)
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