- SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
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Provided is a sulfonamide derivative represented by the following general formula (1) and having an α4 integrin inhibitory effect with high selectivity with a low effect on α4β1 and a high effect on α4β7, or a pharmaceutically acceptable salt thereof (in the general formula (1), A, B, D, E, R41, and a to h are as described in the description).
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Paragraph 0135; 0136; 0137
(2016/09/26)
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- Electrophilic ipso-substitution in uracil derivatives
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Treatment of 5-iodo-1,3,6-trimethyluracil with 50% H2SO 4 gives 1,3,6-trimethyluracil; with 5-bromo-1,3,6-trimethyluracil, a mixture of 1,3,6-trimethyluracil and 6-bromomethyl-1,3-dimethyluracil is obtained. 5-Chloro-1,3,6-trimethyluracil remains inert under these conditions. According to the DFT modeling of the reactions of 5-halo-1,3,6-trimethyluracils, a nucleophilic agent can abstract either Hal+ or the methyl proton from the carbocation formed by protonation of the starting halouracil at position 5, which accounts for the formation of two products from the 5-bromo derivative. Under similar conditions, 6-methyluracil dibromohydrin yields N-bromo-5-bromo-6-hydroxymethyluracil. Bromination or chlorination of 5-hydroxymethyl- or 5-formyl-6-methyluracils follows the ipso-substitution scheme leading to 6-methyluracil 5-halo- and 5,5-dihalohydrins.
- Chernikova,Khursan,Spirikhin,Yunusov
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p. 2445 - 2453
(2014/11/07)
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- 4-Pyrimidinyl-n-acyl-l phenylalanines
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Compounds of Formula I are disclosed, having activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4, and accordingly useful for treating diseases whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.
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- Palladium-Catalyzed Conjugate Addition Type Reaction of 5-Iodopyrimidines with α,β-Unsaturated Ketones
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The reaction of various 5-iodopyrimidines with α,β-unsaturated ketones in the presence of palladium diacetate-triphenylphosphine complex in triethylamine are investigated.In the reaction of 2,4-dialkoxy (or alkylthio)-6-methyl-5-iodopyrimidine the additio
- Wada, Akimori,Ohki, Kazuhiro,Nagai, Sotoo,Kanatomo, Shoichi
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p. 509 - 512
(2007/10/02)
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