170229-80-8Relevant articles and documents
A C=O???Isothiouronium Interaction Dictates Enantiodiscrimination in Acylative Kinetic Resolutions of Tertiary Heterocyclic Alcohols
Greenhalgh, Mark D.,Smith, Samuel M.,Walden, Daniel M.,Taylor, James E.,Brice, Zamira,Robinson, Emily R. T.,Fallan, Charlene,Cordes, David B.,Slawin, Alexandra M. Z.,Richardson, H. Camille,Grove, Markas A.,Cheong, Paul Ha-Yeon,Smith, Andrew D.
supporting information, p. 3200 - 3206 (2018/02/22)
A combination of experimental and computational studies have identified a C=O???isothiouronium interaction as key to efficient enantiodiscrimination in the kinetic resolution of tertiary heterocyclic alcohols bearing up to three potential recognition motifs at the stereogenic tertiary carbinol center. This discrimination was exploited in the isothiourea-catalyzed acylative kinetic resolution of tertiary heterocyclic alcohols (38 examples, s factors up to >200). The reaction proceeds at low catalyst loadings (generally 1 mol %) with either isobutyric or acetic anhydride as the acylating agent under mild conditions.
Compounds useful for treating AIDS
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, (2012/06/30)
The present invention relates to compound (I) for use as an agent for preventing, inhibiting or treating AIDS. The present invention further relates to compounds of formula (I) wherein X is CR0 or N; R0, R1, R2, R3, R4, R7 and R8 independently represent a hydrogen atom, a halogen atom or a group chosen among a (C1-C5)alkyl group, a (C3-C6)cycloalkyl group, a (C1-C5)fluoroalkyl group, a (C1-C5)alkoxy group, a (C1-C5)fluoroalkoxy group, a -CN group, a -COORa group, a -NO2 group, a -NRaRb group, a -NRa-SO2-NRaRb group, a -NRa-SO2-Ra group, a -NRa-C(=O)-Ra group, a -NRa-C(=O)-NRaRb group, a -SO2-NRaRb group, a -SO3H group, a -OH group, a -O-SO2-ORc group, a -O-P(=O)-(ORc)(ORd) group, a -O-CH2-COORc group and can further be a group chosen among: R5 represents a hydrogen atom, a (C1-C5)alkyl group or a (C3-C6)cycloalkyl group; R10 is a hydrogen atom or a chlorine atom, and R11 is a hydrogen atom or a (C1-C4)alkyl group or anyone of its pharmaceutically acceptable salts.