Zobrazeno 1 - 10
of 192
pro vyhledávání: '"and Oljan Repic"'
Publikováno v:
Synthetic Communications. 39:2640-2646
A three-step method for the synthesis of (S)-(1-aza-bicyclo[2.2.2]oct-3-yl)carbamic acid (S)-1-(2-fluorophenyl)ethyl ester HCl salt (12) was developed, starting from alcohol 3 and resulting in an overall yield of 50%. A key feature of the present stu
Publikováno v:
Organic Process Research & Development. 12:1164-1169
A practical synthesis of 1 involving a catalytic enantioselective construction of the quaternary carbon from imine 10 (derived from 13 and 14) and alkyl iodide 5 using Maruoka’s chiral catalyst 11 is described. This asymmetric alkylation followed b
Publikováno v:
Organic Process Research & Development. 12:1137-1141
An optimized convergent synthetic route for the preparation of retinoid X receptor (RXR) antagonist (1) in an overall yield of 35% is described. The formation of the benzodiazepine was achieved in 85% yield using POCl3 in toluene. The drug substance
Autor:
Oljan Repic, Joseph Mckenna, Song Xue, Zhuoliang Chen, Run-Ming Wang, Kapa Prasad, Wen-Chung Shieh
Publikováno v:
Tetrahedron Letters. 49:5359-5362
Our study demonstrated that 4-(4,6-dimethoxy-1,3,5-triazine-2-yl)-4-methyl-morpholinium chloride (DMTMM) is a versatile coupling reagent for the synthesis of sterically-hindered peptidomimetics. It is superior to HBTU/HOBt and CDMT in controlling rac
Publikováno v:
Organic Process Research & Development. 12:183-191
A practical chromatography-free synthesis of an N-formylated hydroxylamine peptide deformylase inhibitor LCD320 is described. A diastereoselective Michael reaction of (4S)-3-[2-(cyclobutylmethyl)-1-oxo-2-propenyl]-4-(phenylmethyl)-2-oxazolidinone wit
Autor:
Guang-Pei Chen, Hui Liu, Calienni John Vincent, David Thomas Parker, Edwin Bernard Villhauer, Thomas J. Blacklock, Oljan Repic, Joginder S. Bajwa, Vivelo James Anthony, Joel Slade, Kapa Prasad
Publikováno v:
Organic Process Research & Development. 11:825-835
An efficient synthesis of a potent insulin-like growth factor I receptor (IGF-IR) inhibitor AEW541 (1) is described. The key step in the synthesis is the cis-selective reductive amination of cyclobutanone, which sets up the desired 1,3-stereochemistr
Autor:
Sushil K. Sharma, Guang-Pei Chen, Christopher Sean Straub, Song Xue, Joseph Mckenna, Xinglong Jiang, Kapa Prasad, Wen-Chung Shieh, Oljan Repic
Publikováno v:
Organic Process Research & Development. 11:711-715
A facile synthesis of octahydro-pyrrolo[2,3-c]pyridine 1 using an intramolecular [3+2]-cycloaddition of an azomethine ylide as the key step and employing DW-therm heat-transfer fluid as a solvent is disclosed. Enantiomerically pure 1 was obtained eit
Publikováno v:
Organic Process Research & Development. 11:769-772
Smopex-111, a commercially available metal-scavenging styryl thiol-grafted polyolefin fiber was treated with palladium acetate giving a reagent with a palladium loading of 4.4−4.7 (wt %). The Pd−Smopex-111 thus generated was found to be a highly
Publikováno v:
Organic Process Research & Development. 11:721-725
An efficient, safe, and cost-effective synthesis of 2-methyltryptamine (2), a key starting material in the synthesis of the histone deacetylase inhibitor LBH589 (1) is described. The reaction of phenylhydrazine (7) with a stoichiometric amount of 5-c
Autor:
Andrew Bach, Oljan Repic, Joseph Mckenna, Thomas J. Blacklock, Liladhar Murlidhar Waykole, Mahavir Prashad
Publikováno v:
Synthetic Communications. 37:1445-1454
Enantioselective syntheses of (R)‐and (S)‐2‐N‐carbomethoxy‐5‐aminoindanes from (R)‐ and (S)‐phenylalanines, respectively, are described. A Friedel–Crafts reaction employing N‐carbomethoxy phenylalanine leads to chiral 2‐N‐carb