Synthesis of novel 5-alkyl/aryl/heteroaryl substituted diethyl 3,4-dihydro-2H-pyrrole-4,4-dicarboxylates by aziridine ring expansion of 2-[(aziridin-1-yl)-1-alkyl/aryl/heteroaryl-methylene]malonic acid diethyl esters

• Satish S. More,
• T. Krishna Mohan,
• Y. Sateesh Kumar,
• U. K. Syam Kumar and
• Navin B. Patel

Beilstein J. Org. Chem. 2011, 7, 831–838, doi:10.3762/bjoc.7.95

• -chloromethylene)malonates 19. The chloro alkenyl malonates 19 were synthesized in two steps from diethyl malonate and acid chlorides. The acylation of diethyl malonate was carried out with various acyl chlorides in the presence of anhydrous magnesium chloride and triethylamine, as per the reaction conditions

• conditions: i) THF, rt, 3 h; ii) NaI, acetone, rt, overnight. Reaction conditions: i) THF, TEA, rt; ii) NaI, acetone, rt, overnight. Synthesis of N-vinylaziridines from diethyl malonate and acyl chlorides. Iodide ion mediated ring expansion of N-vinylaziridines. Supporting Information Supporting Information

Homoallylic amines by reductive inter- and intramolecular coupling of allenes and nitriles

• Peter Wipf and
• Marija D. Manojlovic

Beilstein J. Org. Chem. 2011, 7, 824–830, doi:10.3762/bjoc.7.94

• range of electrophiles to form imine derivatives [28][29][30]. Floreancig and co-workers developed a method for the preparation of α-functionalized amides by trapping N-zirconoimines with acyl chlorides, followed by the addition of nucleophiles to the intermediate acyl imines [31][32][33]. Furthermore

2-Phenyl- tetrahydropyrimidine- 4(1H)-ones – cyclic benzaldehyde aminals as precursors for functionalised β²-amino acids

• Markus Nahrwold,
• Arvydas Stončius,
• Anna Penner,
• Beate Neumann,
• Hans-Georg Stammler and
• Norbert Sewald

Beilstein J. Org. Chem. 2009, 5, No. 43, doi:10.3762/bjoc.5.43

• consists of a 4-DMAP catalysed N-acylation reaction with acyl chlorides and usually affords the target compounds in moderate yields [39][40]. We chose Nα-Cbz-protected β-alanine amide (3) as starting material for the synthesis of the 2-phenyltetrahydropyrimidine-4(1H)-one rac-4 to circumvent the difficulty

Synthesis of the Benzo- fused Indolizidine Alkaloid Mimics

• Daniel L. Comins and
• Kazuhiro Higuchi

Beilstein J. Org. Chem. 2007, 3, No. 42, doi:10.1186/1860-5397-3-42

• biological activity. The various kinds of N-acyldihydropyridones 1 were conveniently prepared from heteroaryl Grignard reagents and N-acylpyridinium salts. Subsequently, dihydropyridones 1 were converted to 8 by use of an intramolecular Heck cyclization. The chloro- and nitro-substituted acyl chlorides 7

Synthesis of phosphorothioates using thiophosphate salts

• Babak Kaboudin and
• Fatemeh Farjadian

Beilstein J. Org. Chem. 2006, 2, No. 4, doi:10.1186/1860-5397-2-4

• and chemoselective thioacylating agent using the reaction of acyl chlorides with dithiophosphoric acid in the presence of pyridine or triethylamine. [51][52][53] In another study we decided to investigate the reaction of the ambident nucleophile ammonium O,O'-diethyl thiophosphate salt with acyl

• chlorides. Reaction of ammonium O,O'-diethyl thiophosphate with benzoyl chloride, as a model compound, in acetonitrile gave benzamide as the major product (Scheme 5). Benzoyl chloride reacts with ammonia (from ammonium O,O'-diethyl thiophosphate) faster than anion O,O'-diethyl thiophosphate to give