- Preparation of 5 - (4 the [...] -bromo methyl-2-biphenyl) - 1-trityl tetrazazole method
-
The invention discloses a method for preparing 5-(4'-bromomethyl-2-biphenyl)-1-triphenyl methyl tetrazole. According to the method, 2-cyano biphenyl is used for replacing 2-cyano 4'-methyl biphenyl in the conventional process and is used as a starting material, and a target product, the 5-(4'-bromomethyl-2-biphenyl)-1-triphenyl methyl tetrazole, is obtained by means of hydroxymethylation, cyclization, protection, and substitution reaction. The method has the advantages of low cost of the raw materials, convenience for recovery of solvent, less comprehensive pollution and the like and is suitable for industrialized production.
- -
-
Paragraph 0035; 0036
(2017/02/24)
-
- Pinacolborane as the boron source in nitrogen-directed borylations of aromatic N, N -dimethylhydrazones
-
A mild procedure for the Ir(III)-catalyzed nitrogen-directed ortho borylation of aromatic N,N-dialkylhydrazones using pinacolborane as the boron source has been developed. The methodology relies on a modified, hemilabile N,N ligand built on a 4-N,N-dimethylaminopyridine unit that provides high reactivity while maintaining exclusive ortho-selectivity. This procedure can be combined with Suzuki-Miyaura cross-couplings in a 'one-pot' fashion to afford functionalized biaryl derivatives that, upon subsequent 'one-pot', high yielding transformations, provide a convenient entry for the preparation of advanced benzonitrile intermediates for the synthesis of Sartan-type drugs.
- López-Rodríguez, Rocío,Ros, Abel,Fernández, Rosario,Lassaletta, José M.
-
p. 9915 - 9920
(2013/01/15)
-
- PROCESS FOR THE PREPARATION OF TETRAZOLE DERIVATIVES FROM ORGANO BORON AND ORGANO ALUMINIUM AZIDES
-
The present invention relates to a method for preparing substituted tetrazoles, compounds obtained according to this method, new reactants and new tetrazole derivatives.
- -
-
Page/Page column 45
(2008/06/13)
-
- Synthesis of Ortho Substituted Arylboronic Esters by in Situ Trapping of Unstable Lithio Intermediates
-
matrix presented Ortho lithiation-in situ boration using lithium 2,2,6,6-tetramethylpiperidide (LTMP) in combination with triisopropylborate (B(OiPr)3) is a highly efficient and experimentally straightforward process for the preparation of ortho substituted arylboronic esters. The mild reaction conditions allow the presence of functionalities such as ester or cyano groups or halogen substituents that are usually not compatible with the conditions used in directed ortho metalation of arenes. The arylboronic esters underwent Suzuki-type cross-coupling with a range of aryl halides, furnishing biaryls in 53-94% yield.
- Kristensen, Jesper,Lysen, Morten,Vedso, Per,Begtrup, Mikael
-
p. 1435 - 1437
(2007/10/03)
-
- Imidazole derivatives having a II antagonist activity
-
Imidazole derivatives having A II antagonist activity, of Formula I, the processes for the preparation thereof, pharmaceutical compositions containing them and the use thereof as therapeutic agents. The described compounds having A II antagonist activity
- -
-
-
- ACYL COMPOUNDS
-
Compounds of the formula STR1 in which R 1 is an aliphatic hydrocarbon radical which is unsubstituted or substituted by halogen or hydroxyl, or a cycloaliphatic or araliphatic hydrocarbon radical; X 1 is CO, SO 2, or--O--C(=O)--with the carbon atom of the carbonyl group being attached to the nitrogen atom shown in formula I; X 2 is a divalent aliphatic hydrocarbon radical which is unsubstituted or substituted by hydroxyl, carboxyl, amino, guanidino or a cycloaliphatic or aromatic radical, or is a divalent cycloaliphatic hydrocarbon radical, it being possible for a carbon atom of the aliphatic hydrocarbon radical to be additionally bridged by a divalent aliphatic hydrocarbon radical; R. sub.2 is carboxyl which, if desired, is esterified or amidated, substituted or unsubstituted amino, formyl which, if desired, is acetalized, 1H-tetrazol-5-yl, pyridyl, hydroxyl which, if desired, is etherified, S(O) m--R where m is 0, 1 or 2 and R is hydrogen or an aliphatic hydrocarbon radical, alkanoyl, unsubstituted or N-substituted sulfamoyl or PO n H 2 where n is 2 or 3; X 3 is a divalent aliphatic hydrocarbon; R 3 is carboxyl, 5-tetrazolyl, SO. sub.3 H, PO. sub.2 H 2, PO 3 H 2 or haloalkylsulfamoyl; and the rings A and B independently of one another are substituted or unsubstituted; in free form or in salt form, can be prepared in a manner known per se and can be used, for example, as medicament active ingredients.
- -
-
-