- Novel commercial scale synthetic approach for 5-cyanoindole: A potential intermediate for vilazodone hydrochloride, an antidepressant drug
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Present work describes the synthesis of 5-cyanoindole, a common intermediate used in various synthetic route of the antidepressant vilazodone hydrochloride. The protocol is both robust and commercially viable, utilizing readily available and low-cost materials and the isomers are environmental friendly than previously reported routes through its evading use of cyanide reagents and heavy metals.
- VENKATANARAYANA,NUCHU, RAVI,SHARATH BABU,GARREPALLI, GANGA SRAVANTHI,TANGALLAPALL, SUDHAKAR
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p. 2460 - 2462
(2020/10/22)
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- DIHYDROBENZOFURAN DERIVATIVES AS INSECTICIDAL COMPOUNDS
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The present invention relates to compounds of formula (I) wherein Q is (Q1) or (Q2) G1 is oxygen or sulfur; Y1 is oxygen, sulfur or CH2; Y2, Y3 and Y4 are each independently C-H, C-R5 or nitrogen, wherein no more than one of Y2, Y3 and Y4 is C-R5; Y5 is hydrogen, halogen, C1-C8alkyl, C1-C8haloalkyl or C3-C8cycloalkyl; Y6 is hydrogen, halogen, cyano, C1-C8alkyl, C1-C8haloalkyl or C3-C8cycloalkyl; R1a is hydrogen, C1-C8alkyl, C1-C8alkoxy, C1-C8alkylcarbonyl or C1-C8alkoxycarbonyl; R1b is hydrogen, C1-C8alkyl, C1-C8alkylcarbonyl or C1-C8alkoxycarbonyl; R3 is C1-C8haloalkyl; R4 is aryl or aryl substituted by one to five R10, or heteroaryl or heteroaryl substituted by one to five R10; R6a is hydrogen, cyano, C1-C8alkyl, C1-C8haloalkyl or C3-C8cycloalkyl; R6b is hydrogen, cyano, C1-C8alkyl, C1-C8haloalkyl or C3-C8cycloalkyl; or R6a and R6b together with the carbon atom to which they are attached may form a 3 to 6-membered carbocyclic ring; and R2a, R2b, R and R are as defined in the claims. The invention also relates to methods of controlling insects, acarines, nematodes or molluscs which comprises applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest an insecticidally, acaricidally, nematicidally or molluscicidally effective amount of a compound of formula I.
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- Nitration of moderately deactivated arenes with nitrogen dioxide and molecular oxygen under neutral conditions. Zeolite-induced enhancement of regioselectivity and reversal of isomer ratios
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In the presence of zeolites, moderately deactivated arenes such as 1-nitronaphthalene, naphthonitriles, and methylated benzonitriles can be smoothly nitrated at room temperature by the combined action of nitrogen dioxide and molecular oxygen. The regioselectivity is considerably improved as compared with the conventional nitration methodology based on nitric and sulfuric acids. In some cases, the minor isomer became favoured to a significant extent, resulting in the reversal of ordinary isomer ratios of nitration products.
- Peng, Xinhua,Fukui, Naoyuki,Mizuta, Masayuki,Suzuki, Hitomi
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p. 2326 - 2335
(2007/10/03)
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- Use of conformationally restricted benzamidines as arginine surrogates in the design of platelet GPIIb-IIIa receptor antagonists
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The use of 5,6-bicyclic amidines as arginine surrogates in the design of a novel class of potent platelet glycoprotein IIb-IIIa receptor (GPIIb-IIIa) antagonists is described. The additional conformational restriction offered by the bicyclic nucleus results in 20-400-fold increases in potency compared to the freely flexible, acyclic benzamidine counterpart. The design, synthesis, structure-activity relationships (SAR), and in vitro activity of this novel class of GPIIb-IIIa antagonists are presented.
- Sall, Daniel J.,Arfsten, Ann E.,Bastian, Jolie A.,Denney, Michael L.,Harms, Cathy S.,McCowan, Jefferson R.,Morin Jr., John M.,Rose, Jack W.,Scarborough, Robert M.,Smyth, Mark S.,Um, Suzane L.,Utterback, Barbara G.,Vasileff, Robert T.,Wikel, James H.,Wyss, Virginia L.,Jakubowski, Joseph A.
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p. 2843 - 2857
(2007/10/03)
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- 5,6-Bicyclic glycoprotein IIb IIIa antagonists useful in inhibition of platelet aggregation
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This invention relates to 5,6 fused ring bicyclic compounds inclusive of indoles, benzofurans, and benzothiophenes, and corresponding to the formula (I) substituted with both basic (B) and acidic (A) functionality, which are useful in inhibition of platelet aggregation.
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- Anthelmintically active benzenepropanamide derivatives
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This invention is directed to a method for treating helminthiasis in an animal which method comprises administering to an animal in need thereof an anthelmintically effective amount of a compound of the Formula (I): STR1 wherein Z is oxygen or sulfur;R 1 is hydrogen or lower alkyl; andR 2, R 3, R 4 and R 5 are independently hydrogen, halo, lower haloalkyl, lower alkoxy, lower haloalkoxy, nitro, cyano, halophenoxy, haloalkylphenoxy, thiocyano or isothiocyano, provided that R 2 and R 3 cannot simultaneously be hydrogen and that R 4 and R 5 cannot simultaneously be hydrogen; or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions formulated therewith. This invention is also directed to novel anthelmintically active benzenepropanamides of Formula (I) wherein Z is oxygen.
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- GRIGNARD REAGENTS SELECTIVE ATTACK TO NITROARENIC FUNCTION IN THE PRESENCE OF OTHER ELECTROPHILIC GROUPS
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Exclusive alkylation of the nitroarenic system takes place in competitive reactions of RMgX with nitrobenzene and various electrophiles such as ketones, esters, cyanoand iodo-derivatives and in reactions with some functionalized nitrobenzenes, only aldehy
- Bartoli, G.,Bosco, M.,Dalpozzo, R.
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p. 115 - 118
(2007/10/02)
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