Zobrazeno 1 - 10
of 45
pro vyhledávání: '"JOSEPH E. LYNCH"'
Publikováno v:
Tetrahedron. 63:4459-4463
An efficient asymmetric synthesis of selective estrogen receptor β-modulator (S)-4-bromo-9a-butyl-8-chloro-6-fluoro-7-hydroxy-1,2,9,9a-tetrahydro-fluoren-3-one was developed. The route features a chemoselective aromatic chlorination reaction, an asy
Publikováno v:
Organic Process Research & Development. 10:398-402
An expedient regioselective synthesis of a GABA α2/3 agonist 1 is described. The key step is an efficient regioselective palladium-catalyzed coupling of 7-trifluoromethylimidazo[1,2-a]pyrimidine (5) to 5‘-chloro-4,2‘-difluorobiphenyl-2-carbonitr
Autor:
Michael B. Hicks, Vincent Antonucci, George Zhou, Joseph E. Lynch, Mark Cameron, Yao-Jun Shi, David R. Lieberman, Zhihong Ge
Publikováno v:
Journal of Pharmaceutical Sciences. 92:529-535
A simple and safe prototype apparatus was designed and adapted for the in situ determination of the moisture content of a cytotoxic compound (9-fluorenylmethyl-protected doxorubicin-peptide conjugate, or Fm-DPC) by near-infrared absorbance spectrosco
Autor:
Mark Cameron, Yao-Jun Shi, Paul J. Reider, Robert A. Reamer, Michael A. Robbins, Joseph E. Lynch, David R. Lieberman, Ralph P. Volante, Ulf H. Dolling
Publikováno v:
Synlett. :0647-0650
An efficient synthesis of the sodium salt of the doxorubicin-peptide conjugate 1, useful for the treatment of prostate cancer is described. The EDC-mediated amide formation between the heptapeptide 4 and doxorubicin (2) as the key step has been exten
Autor:
Ashok Maliakal, Joseph E. Lynch, Philip J. Pye, Ralph P. Volante, Paul J. Reider, Woo-Baeg Choi, Yao-Jun Shi, Kenneth M. Wells, Kai Rossen, Hywyn R.O. Churchill, Jess Sager
Publikováno v:
Tetrahedron. 55:909-918
A highly convergent, asymmetric synthesis of L-768,673, an I ks Class III antiarrythmic drug candidate, is described. Synthesis of the recemic 1-trifluoroethyl-3-amino-5-phenyl benzodiazepinone [(±)-amine] was achieved by Ru-catalyzed hydrogenation
Publikováno v:
Tetrahedron Letters. 39:3679-3682
The use of cis -aminoindanol as a chiral auxiliary for asymmetric synthesis of α-amino acids is described. Alkylation of the chirally modified glycine enolate 2 with a number of alkyl halides in the presence of lithium chloride gave the correspondin
Autor:
W.-B. Choi, and Robert A. Reamer, Hywyn R.O. Churchill, Ralph P. Volante, Richard G. Ball, Joseph E. Lynch
Publikováno v:
The Journal of Organic Chemistry. 62:9223-9228
An asymmetric synthesis of the PDE IV inhibitor, CDP840 (3) is reported. The absolute stereochemistry was controlled by a Jacobsen epoxidation of the Z triaryl olefin 8 (89% ee) or the E triaryl olefin 9 (48% ee). The disparate results in stereocontr
Autor:
Kai Rossen, Ralph P. Volante, David Askin, Robert A. Reamer, Joseph E. Lynch, Veena Upadhyay, Paul J. Reider, Kenneth M. Wells, Ioannis N. Houpis, Jess Sager, Peter G. Houghton, Audrey Molina, Peter E. Maligres
Publikováno v:
Tetrahedron. 53:10983-10992
The preparation of the Merck Growth Hormone Secretagogue; MK-677 is described. A Fischer indole/reduction based strategy provides the novel spiroindoline nucleus of this potent compound. This optimized sequence necessitates the isolation of only one
Autor:
Ralph P. Volante, Yao Jun Shi, Paul J. Reider, Guy R. Humphrey, Kenneth M. Wells, Joseph E. Lynch
Publikováno v:
Tetrahedron Letters. 37:6439-6442
Regioselective nucleophilic substitutions of tri- and di-substituted fluorobenzoates, fluorobenzonitriles, and fluoronitrobenzenes were accomplished by sequential addition of various nucleophiles, such as, potassium N-Boc-4-piperidinyl oxide, potassi
Publikováno v:
The Journal of Organic Chemistry. 61:6425-6429