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Synthesis of 5-Amino and 3,5-Diamino Substituted 1,2,4-Thiadiazoles by I2-Mediated Oxidative N–S Bond Formation

10.1021/acs.joc.7b00814

2017-05-12

An oxidative N–S bond formation reaction has been established for 1,2,4-thiadiazole synthesis employing molecular iodine as the sole oxidant. The features of the present reaction include no use of transition metals, mild reaction conditions, simple operation,...

The Synthesis of Chiral β,β-Diaryl Allylic Alcohols and Their Use in the Preparation of α-Tertiary Allylamines and Quaternary α-Amino Acids

10.1021/acs.joc.7b00475

2017-05-11

An approach to nonracemic β,β-diarylsubstituted allyl alcohols is described. Their synthesis starts from l-lactic acid-derived propargyl alcohol, which is submitted to sequential Sonogashira/Suzuki or Sonagashira/Stille coupling reactions. Both approaches ena...

Total Synthesis of γ-Indomycinone and Kidamycinone by Means of Two Regioselective Diels–Alder Reactions

10.1021/acs.joc.7b00544

2017-05-11

An efficient access for the synthesis of pluramycinones is described. Total syntheses of racemic γ-indomycinone and kidamycinone were achieved by means of two Diels–Alder reactions. A first Diels–Alder condensation followed by a Stille cross-coupling is used ...

Unexpected Observation of the Dimroth Rearrangement in the Ribosylation of 4-Aminopyrimidines

10.1021/acs.joc.7b00780

2017-05-11

A method for the preparation of 1-(N-ribofuranosyl)-6-imino-1,6-dihydropyrimidin-4-amines 3 or 4-(N-ribofuranosyl)-6-aminopyrimidines 4 via glycosylation of 4-aminopyrimidines 2 or 5 is described. Silylated 4-aminopyrimidines 2 or 5 upon ribosylation with 1 p...

Theoretical Study of the BF3-Promoted Rearrangement of Oxiranyl N-Methyliminodiacetic Acid Boronates

10.1021/acs.joc.7b01096

2017-05-11

The mechanism of the rearrangement of oxiranyl N-methyliminodiacetyl (MIDA) boronates in dicholoromethane has been extensively investigated with density functional theory. Several reaction pathways were examined. Our results revealed that the most-favorable m...

Impact of Conjugation and Hyperconjugation on the Radical Stability of Allylic and Benzylic Systems: A Theoretical Study

10.1021/acs.joc.7b00549

2017-05-11

Resonantly stabilized radicals are some of the most investigated chemical species due to their preferential formation in a wide variety of chemical environments. Density functional theory and post-Hartree–Fock calculations were utilized to elucidate the chemi...

Copper-Catalyzed Functionalizations of C60 with Amino Alcohols

10.1021/acs.joc.7b00741

2017-05-11

CuI-catalyzed diverse functionalizations of C60 with amino alcohols with aerobic oxygen as the sole oxidant have been explored. For 2-/3-amino alcohols, an aminooxygenation reaction occurs to generate fulleromorpholine and fullerooxazepane derivatives. When a...

Chemoselective Reduction of Azlactones Using Schwartz’s Reagent

10.1021/acs.joc.7b00820

2017-05-11

Highly chemoselective addition of Schwartz’s reagent to widely available azlactones is described. This method allows the preparation of challenged functionalized α-amino aldehydes, in good to high isolated yields at room temperature, after only 2 min reaction...

Synthesis of 4-Halo-3(2H)-furanones Using Intramolecular Cyclization of Sulfonium Salts

10.1021/acs.joc.7b00399

2017-05-11

A simple and efficient synthesis of 4-halo-3(2H)-furanones by halogenative intramolecular cyclization of sulfonium salts is described, which can expedite the production of a variety of 4-bromo- or 4-iodo-3(2H)-furanones, useful synthetic building blocks, in g...

Svetamycins A–G, Unusual Piperazic Acid-Containing Peptides from Streptomyces sp.

10.1021/acs.joc.7b00228

2017-05-10

Seven new halogenated peptides termed svetamycins A–G (1–7) have been isolated from laboratory cultures of a Streptomyces sp. Svetamycins A–D, F, and G are cyclic depsipeptides, whereas svetamycin E is a linear analogue of svetamycin C. Their structures were ...