- Heterocyclization and Spirocyclization Processes Based on Domino Reactions of N-Tosylhydrazones and Boronic Acids Involving Intramolecular Allylborylations of Nitriles
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Polycyclic molecules featuring all-carbon quaternary bridgehead centers were synthesized through domino cyclizations between N-tosylhydrazones and boronic acids. Variations of the general cascade have been applied for the preparation of 3-quinuclidinones and related alkaloid-like scaffolds through transannular heterocyclizations. Moreover, the employment of 3-cyanopropyl and 4-cyanobutylboronic acids and α,β-unsaturated N-tosylhydrazones led to spirocycles through unprecedented formal [n+1] cyclizations, including the stereoselective spirocyclization of the Hajos–Parrish ketone. The common feature of all the new reactions described is the creation of an all-carbon quaternary center by formation of two Csp3?C bonds on the hydrazonic carbon atom. DFT-based calculations suggested the occurrence of cascade processes, which involve a diazo compound carboborylation followed by a 1,3-borotropic rearrangement on an intermediate allylboronic acid and a novel bora-aza-ene cyclization.
- Plaza, Manuel,Parisotto, Stefano,Valdés, Carlos
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supporting information
p. 14836 - 14843
(2018/09/25)
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- COMPOUNDS AS CRTH2 ANTAGONIST AND USES THEREOF
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The compounds of Formula (I) which can be used as CRTH2 receptor antagonists are provided. The compounds of Formula (I) can be used in the treatment and prevention of asthma, allergic rhinitis and atopic dermatitis, as well as other diseases mediated by prostaglandin D2 (PGD2) at the CRTH2 receptor.
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Paragraph 00457
(2016/04/20)
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- IMPROVED PROCESS FOR PREPARING 2-[(2E)-2-FLUORO-2-(3-PIPERIDINYLIDENE)ETHYL]-1H-ISOINDOLE-1,3(2H)-DIONE
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The present invention relates to an improved process for preparing 2-[(2E)-2-fluoro-2-(3-piperidinylidene)ethyl]-1H-isoindole-1,3(2H)-dione, or a salt thereof, which is an intermediate in the synthesis route of the antibacterial compound 7-[(3E)-3-(2-amin
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Page/Page column 14
(2013/04/13)
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- Lightening Agents and/or Dyes that Contain Aldehyde(s)
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Agents for dyeing and/or lightening keratin fibers, in particular human hair, containing, relative to the weight thereof, 0.001 to 15 wt. % of at least one aldehyde of the formula (I): wherein X represents —CH(R2)—SO2—Y—R1, —CR3R4R5, or wherein Y represents —CH(CHO)— or —CH2— or a chemical bond, and wherein each of R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 independently represents —H or —CN or —F or —Cl or —Br or —I or —CHO or —NH2 or —NO2 or —CF3 or —CCl3 or —CF2CF3 or —CCl2CCl3 or an optionally substituted (C1-C6) alkyl group or a hydroxyalkyl group or a polyhydroxyalkyl group or an optionally substituted (C1-C6) alkylene group, and wherein the agent contains no oxidation dye precursors of developer and coupler type.
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