Indium(III) chloride is an effective Lewis acid catalyst for one-pot allylation–etherification and reductive etherification of aromatic aldehydes with functional silanes, allyltriethoxysilane, and triethoxysilane, at room temperature to afford corresponding ethers in excellent yields. Additionally, the InCl3-catalyzed reactions in the presence of TMSCl offer significant advantages in its ease of working-up
[EN] PREPARATION OF QUETIAPINE<br/>[FR] PREPARATION DE QUETIAPINE
申请人:FERMION OY
公开号:WO2005028457A1
公开(公告)日:2005-03-31
The present invention discloses a process for the preparation of quetiapine, which comprises the reaction of dibenzo[b,f][1,4]thiazepin-11-ylamine with a compound of the general formula (II) as well as novel intermediates in the process.
A process is disclosed for preparing bidentate ligands of the formula:
wherein:
each of Ar, R′, R˝ and Y are specifically defined species;
the x bonds and the y bonds are attached to adjacent carbon atoms on the ring structures; and
n is a whole number in the range of 0-4 where Ar is phenyl: 0-6 where Ar is naphthyl: and 0-8 where Ar is phenanthryl or anthracenyl.
The invention process comprises
a. reductively coupling an ortho-substituted aromatic moiety to produce a biphenyl compound;
b. contacting the biphenyl compound produced in Step (a) with an anion having the structure:
wherein Y, Y′ and R′ are specifically defined species;
under conditions appropriate to form said bidentate ligand or the dioxide precursor thereof; and
c. optionally reducing the intermediate product when the oxy-anion,
is employed as the anion in Step (b).
A method for the preparation of biaryl compounds is disclosed which comprises contacting an aryl halide under conditions suitable to form a Grignard reagent and thereafter contacting the Grignard reagent with an aryl chloride in the presence of a catalyst comprising a nickel compound and a coordinating ligand under conditions suitable for the formation of biaryl compound. In an alternate embodiment of the present invention, biaryl compounds are prepared directly from aryl halides in a single reaction vessel by contacting aryl halide with elemental magnesium and a nickel catalyst comprising a nickel compound and a coordinating ligand in an aprotic, non-polar, ether-containing solvent system for a time and under conditions suitable for the formation of biaryl compound.
The present invention provides a novel compound having an antiviral action, in particular, an HIV replication inhibiting action, as well as a pharmaceutical composition, in particular, an anti-HIV agent.
wherein, a broken line means the presence or absence of a bond; R1 is substituted or unsubstituted alkyl etc., R2 is substituted or unsubstituted alkyloxy etc.; n is 1 or 2; R3 is a substituted or unsubstituted aromatic carbocyclic group; R4 is a hydrogen atom etc.; R5 is a substituted or unsubstituted aromatic carbocyclic group etc.; Y is a single bond etc.; R6 is substituted or unsubstituted alkyl; R7 is -Z-R71 etc.; Z is - NR72-CO- etc.; R71 is substituted or unsubstituted alkyl etc.; R72 is a hydrogen atom etc.