Sulfur-promoted,one-pot,and metal-free conversion of aromatic aldehydes to nitriles using an inorganic ammonium salt as the nitrogen source

A simple protocol for the sulfur-promoted conversion of aromatic aldehydes to aromatic nitriles has been developed.This strategy enables the one-pot conversion of inexpensive and readily available aromatic aldehydes into highly valuable aromatic nitriles using a cheap inorganic ammonium salt as the nitrogen source in the absence of metals.Significantly,a broad scope of substrates was explored using this strategy,and various groups,including alkyl,alkoxyl,alkylthiol,hydroxyl,amino,aryl,alkenyl,cyano,carboxyl,and borate ester groups were tolerated,and good to excellent yields were achieved in most cases.Additionally,polycyclic aromatic aldehydes and heteroaromatic aldehydes also could be converted to the corre-sponding nitriles with satisfactory yields.This method can be utilized as a powerful tool for the cyanation of complex molecules.

Association between SLC17A7 gene polymorphisms and venlafaxine for major depressive disorder in a Chinese Han population:a prospective pharmacogenetic case-control study

Objective: Venlafaxine is a common antidepressant and its therapeutic effect varies among people with different genetic backgrounds. The aim of this study was to investigate whether single nucleotide polymorphisms (SNPs) in theSLC17A7 gene are associated with the treatment outcome of venlafaxine in a Chinese Han population with major depressive disorder.Methods: This prospective pharmacogenetic case-control study that involved genotyping of four SNPs ofSLC17A7 was conducted on 175 major depressive disorder patients of Chinese Han origin, aged 18 to 65 years, participated in the study from April 2005 to September 2006. Comparisons of allele and genotype frequencies of all SNPs were performed between the responder/remission group and the nonresponder/nonremission group. This study was approved by the Institutional Ethics Committee of Sichuan University (approval No. 20151112-265).Results: The allele and genotype frequencies of the four candidate SNPs inSCL17A7 showed no significant difference between responders and nonresponders. Meanwhile, no significant difference was detected in the four investigatedSLC17A7 SNPs between patients who did and did not exhibit remission. Although one of the investigatedSLC17A7 variants (rs1578944) demonstrated a significant association (P=0.022) with a response to venlafaxine after 6 weeks of treatment in the survival analysis, the association was unclear after a Bonferroni multiple comparisons test was conducted.Conclusion: No significant association exists between the four candidate SNPs (rs1043558, rs1320301, rs1578944, and rs74174284) inSLC17A7 and venlafaxine treatment in the Chinese Han population.

Synthesis of benzisothiazoles by a three-component reaction using elemental sulfur and ammonium as heteroatom components under transition metal-free conditions

A strategy for the synthesis of benzisothiazoles by a three-component reaction was developed using elemental sulfur and ammonium as heteroatom components under transition metal-free conditions.The reaction is preferably based on pyridine or quinoline ring substrate,and good to excellent yields can be obtained.Notably,this reaction has been applied to the gram-scale synthesis of bioactive molecules.