78906-11-3

The invention relates to a method for synthesizing 2 - hydroxy isopropyl substituted acetophenone method, it includes S1: in the 130 - 140 °C temperature, will be acetyl benzoic acid methyl ester and ethylene glycol in the organic solvent and the presence of a catalyst under the conditions of the reaction, generating comprises intermediate reaction mixture 1st; S2: the 1st reaction mixture is cooled to room temperature, the reaction mixture purification 1st, get midbody; S3: in - 5 to 0 °C temperature, in an inert atmosphere environment, the intermediate of the tetrahydrofuran solution dripped into methyl bromide in tetrahydrofuran solution of the magnesium oxide, the method comprises generating the 2 - hydroxy isopropyl substituted acetophenone 2nd reaction mixture; and S4: purifying the 2nd reaction mixture, to obtain the 2 - hydroxy isopropyl substituted acetophenone; wherein said alkali comprises acyl benzoic acid methyl ester 4 - acetyl benzoic acid methyl ester or 3 - acetyl-benzoic acid methyl ester. The methods of the invention and is simple, preparation procedure is simple and convenient, high yield, small pollution to the environment. (by machine translation)

The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.

The development of an unprecedented chemoselective transformation has contributed to forming a novel synthetic process for target molecules. Chemoselective oxidation of aromatic acetals has been accomplished using a reusable palladium on carbon catalyst under atmospheric oxygen conditions to form ester derivatives with tolerance of aliphatic acetals and ketals.

The present invention provides tricyclic compounds according to formula (I): (I) where R1, R2, R3, W, X, Y, Z, m, n, and p are as defined in the description; as well as pharmaceutical compositions comprising the same, meth

A range of aryl bromides undergo Heck reaction with ethylene glycol vinyl ether, in the presence of [PdCl(C3H5)]2/ cis,cis,cis-1,2,3,4-tetrakis[(diphenylphosphanyl)methyl]cyclopentane as catalyst, to give regioselectively protected arylacetaldehydes in good yields. The β-arylation products were obtained in with 93-100 % selectivity with electron-poor aryl bromides or heteroaryl bromides. Furthermore, this catalyst can be used at low loading, even for reactions with sterically hindered aryl bromides. The aryl vinyl ether intermediates undergo subsequent ketalisation to give the corresponding 2-benzyl-1,3-dioxolane derivatives. Wiley-VCH Verlag GmbH & Co. KGaA, 2006.