0000000001314400
AUTHOR
Thomas Mathew
Direct Difluorination–Hydroxylation, Trifluorination, and C(sp2)–H Fluorination of Enamides
A direct double functionalization involving both difluorination and hydroxylation of enamides is reported. With the appropriate combination of an electrophilic fluorinating reagent and H2O, the most convenient and ecofriendly hydroxylating agent, the preparation of 3-(difluoroalkyl)-3-hydroxyisoindolin-1-ones was achieved under basic or Bronsted acidic conditions. Suitable conditions for trifluorination as well as C(sp2)–H fluorination were also identified. Subsequent asymmetric functionalization of the obtained gem-difluorinated products has also been demonstrated.
Synthesis of 3-substituted isoindolin-1-ones via a tandem desilylation, cross-coupling, hydroamidation sequence under aqueous phase-transfer conditions
A simple and expedient method for the synthesis of 3-methylene-isoindolin-1-ones 4 under aqueous phase-transfer conditions has been developed. Starting from 2-iodobenzamides 1 and (silyl) alkynes, the products are obtained in high yields and short reaction times (30 min) with the use of inexpensive CuCl/PPh3 catalyst system in the presence of n-Bu4NBr (TBAB) as a phase-transfer agent. Terminal alkynes are conveniently "unmasked" upon in situ desilylation under the reaction conditions. Alkynes possessing heterocyclic moieties were also found as amenable substrates. Furthermore, a one-pot process starting from 2-iodobenzamides 1, aryl halides (bromides or iodides) and trimethylsilylacetylene …
Benzodiazines: recent synthetic advances.
Benzodiazines (diazonaphthalenes with both nitrogens in the same ring) – cinnolines (1,2-benzodiazine), quinazolines (1,3-benzodiazine), phthalazines (2,3-benzodiazine) and quinoxalines (1,4-benzodiazine) – are important class of compounds with broad biological properties and wide application in pharmaceutical as well as agrochemical arenas. These diazaheterocycles are present in a wide variety of bioactive natural products as well as synthetic molecules that are good drug candidates constituting key structural units responsible for their pronounced therapeutic activities. Their rapidly growing uses and applications in medicinal and agrochemical arenas prompt the researchers for further stu…
ChemInform Abstract: Synthesis of 3-Substituted Isoindolin-1-ones via a Tandem Desilylation, Cross-Coupling, Hydroamidation Sequence under Aqueous Phase-Transfer Conditions.
A simple and expedient method for the synthesis of 3-methylene-isoindolin-1-ones 4 under aqueous phase-transfer conditions has been developed. Starting from 2-iodobenzamides 1 and (silyl)alkynes, the products are obtained in high yields and short reaction times (30 min) with the use of inexpensive CuCl/PPh3 catalyst system in the presence of n-Bu4NBr (TBAB) as a phase-transfer agent. Terminal alkynes are conveniently “unmasked” upon in situ desilylation under the reaction conditions. Alkynes possessing heterocyclic moieties were also found as amenable substrates. Furthermore, a one-pot process starting from 2-iodobenzamides 1, aryl halides (bromides or iodides) and trimethylsilylacetylene (…
Inference for the interclass correlation in familial data using small sample asymptotics
Inference on the parent-offspring correlation coefficient is an important problem in the analysis of familial data, and point estimates and likelihood based inference are available in the literature. In this work, corrections for the signed log-likelihood ratio test statistics are proposed, based on small sample asymptotics, in order to achieve accurate small sample performance. The corrected statistic can be used for hypothesis testing as well as for interval estimation.
CCDC 1427402: Experimental Crystal Structure Determination
Related Article: Socrates B. Munoz, Alexandra N. Aloia, Alexander K. Moore, Attila Papp, Thomas Mathew, Santos Fustero, George A. Olah, G. K. Surya Prakash|2016|Org.Biomol.Chem.|14|85|doi:10.1039/C5OB02187A
CCDC 1426924: Experimental Crystal Structure Determination
Related Article: Socrates B. Munoz, Alexandra N. Aloia, Alexander K. Moore, Attila Papp, Thomas Mathew, Santos Fustero, George A. Olah, G. K. Surya Prakash|2016|Org.Biomol.Chem.|14|85|doi:10.1039/C5OB02187A