Synthesis of 2(1H)-Pyrimidinone-Containing .ALPHA.-Amino Acid Derivatives by Chemical Modification of L-Glutamic Acid.

One Pot Synthesis of Alpha-Aminonitrile and Alpha-Amino Acid From Schiff Bases

Addition of Potassium cyanide to a mixture of Schiff base and lithium perchlorate afforded a-aminonitriles in high yields. Addition of potassium cyanide to a methanolic solution of Schiff base and phosphoric acid afforded a-aminonitriles. When the reaction mixture was refluxed it gave a-amino acids in high yields.

Stereocontrolled synthesis of 5-azaspiro[2.3]hexane derivatives as conformationally “frozen” analogues of L-glutamic acid

Several strategies aimed to "freeze" natural amino acids into more constrained analogues have been developed with the aim of enhancing in vitro potency/selectivity and, more in general, drugability properties. The case of L-glutamic acid (L-Glu, 1) is of particular importance since it is the primary excitatory neurotransmitter in the mammalian central nervous system (CNS) and plays a critical r...

The synthesis of some peptides containing glutamic acid.

Amino acid derivatives. Part I. Synthesis, antiviral and antitumor evaluation of new alpha-amino acid esters bearing coumarin side chain.

A series of amino acid esters bearing coumarin (3-15) were synthesized and evaluated, in vitro, against HIV-1, and bovine viral diarrhea virus (BVDV). The in vitro cytotoxicity of 3-10 and 12 was assayed against a panel of tumor cell lines consisting of CD4 human T-cells. Compound 14 showed inhibition of HIV-1 with EC50 > 1.6 microg mL(-1), meanwhile compound 9 exhibited activity against leukae...

Synthesis of arylidinebarbituric acid derivatives catalyzed by dodecylbenzenesulfonic acid (DBSA) in aqueous media

A series of arylidine barbituric acid derivatives was synthesized by Knoevenagel condensation reaction of aromatic aldehydes with barbituric acid or thiobarbituric acid using dodecylbenzenesulfonic acid as a Brønsted acid-surfactant catalyst in aqueous media. Regardless of the nature of the substitution (electron-donating and -withdrawing), all the reactions were completed within 15-65 min in w...