The invention relates to an improved process for the manufacture of bis-resorcinyl triazines of formula (I) wherein R.sup.1 is a C.sub.1C.sub.18alkyl group or C.sub.2-C.sub.18alkenyl group as well as the respective alkyl substituted bis-resorcinyl derivatives of formula (II) wherein R.sup.1 is a C.sub.1-C.sub.18alkyl group or C.sub.2-C.sub.18alkenyl group and R.sup.2 and R.sup.3 are independently of each other a C.sub.1-C.sub.18alkyl group or a C.sub.2-C.sub.18alkenyl group.

##STR00001##

The invention relates to an improved process for the manufacture of bis-resorcinyl triazines of formula (I) wherein R.sup.1 is a C.sub.1C.sub.18alkyl group or C.sub.2-C.sub.18alkenyl group as well as the respective alkyl substituted bis-resorcinyl derivatives of formula (II) wherein R.sup.1 is a C.sub.1-C.sub.18alkyl group or C.sub.2-C.sub.18alkenyl group and R.sup.2 and R.sup.3 are independently of each other a C.sub.1-C.sub.18alkyl group or a C.sub.2-C.sub.18alkenyl group.

##STR00001##

The present invention relates to a method for preparing a citalopram diol represented by formula IV, comprising the following steps: in the existence of an auxiliary reagent of metal salt, allowing 5-cyanophthalide to sequentially subjected to Grignard addition reactions with p-fluorophenyl magnesium halide and N, N-dimethylaminopropyl magnesium halide in an organic solvent; and after the reactions are completed, performing hydrolysis and separation to obtain citalopram diol represented by formula IV. In the present invention, by adding an auxiliary reagent of metal salt, the activity and the selectivity of the Grignard reactions are remarkably improved, and the reaction yield is obviously enhanced.

##STR00001##

The present invention relates to a method for preparing a citalopram diol represented by formula IV, comprising the following steps: in the existence of an auxiliary reagent of metal salt, allowing 5-cyanophthalide to sequentially subjected to Grignard addition reactions with p-fluorophenyl magnesium halide and N, N-dimethylaminopropyl magnesium halide in an organic solvent; and after the reactions are completed, performing hydrolysis and separation to obtain citalopram diol represented by formula IV. In the present invention, by adding an auxiliary reagent of metal salt, the activity and the selectivity of the Grignard reactions are remarkably improved, and the reaction yield is obviously enhanced.

##STR00001##

Oleanolic acid methyl ester derivatives demonstrate potent anti-diabetic activities. In in vitro anti-diabetic testing, the derivatives showed more potency regarding dipeptidyl peptidase-4 (DPP-IV) inhibitor activity, peroxisome proliferator-activated receptors (PPARs) agonist activity, and -Glucosidase inhibitors activity, as compared to reference standards oleanolic acid and acarbose. In in vivo oral hypoglycemic testing, both acute and sub-acute studies demonstrated that the derivatives had high potency and long duration of action compared to the reference standards pioglitazone, acarbose and oleanolic acid.

Oleanolic acid methyl ester derivatives demonstrate potent anti-diabetic activities. In in vitro anti-diabetic testing, the derivatives showed more potency regarding dipeptidyl peptidase-4 (DPP-IV) inhibitor activity, peroxisome proliferator-activated receptors (PPARs) agonist activity, and -Glucosidase inhibitors activity, as compared to reference standards oleanolic acid and acarbose. In in vivo oral hypoglycemic testing, both acute and sub-acute studies demonstrated that the derivatives had high potency and long duration of action compared to the reference standards pioglitazone, acarbose and oleanolic acid.

The present invention relates to a series of analogues of natural product Pyripyropene A represented by general formula I and a preparation method and use thereof. More particularly, the present invention relates to analogues of the natural product Pyripyropene A, a preparation method and use thereof as the acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors for the treatment of cardiovascular diseases such as atherosclerosis and the like.

##STR00001##

An organomagnesium synthesis agent, a process for preparing this synthesis agent, and its use.

An organomagnesium synthesis agent, a process for preparing this synthesis agent, and its use.

The present disclosure provides methods of manufacturing psilocybin and crystalline psilocybin via a reaction of psilocin and tetrabenzylpyrophosphate in the presence of lithium chloride complex Grignard reagent, which is followed by hydrogenation. Methods of producing psilocin from 4-hydroxyindole or 4-acetoxyindole are also provided.