Zobrazeno 1 - 10
of 35
pro vyhledávání: '"Nicholas A. Magnus"'
Diastereoselective Pictet-Spengler Based Synthesis of a Chiral Tetrahydroisoquinoline D1 Potentiator
Publikováno v:
The Journal of organic chemistry. 85(11)
A practical synthesis of a D1 potentiator chiral tetrahydroisoquinoline has been accomplished employing diastereoselective Pictet-Spengler methodology to access the required trans-stereochemistry. A dynamic kinetic resolution by crystallization gives
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::96a92e691b37c81def6dd137fb254b89
https://pubmed.ncbi.nlm.nih.gov/32402198
https://pubmed.ncbi.nlm.nih.gov/32402198
Publikováno v:
The Journal of organic chemistry. 82(12)
An efficient three-step synthesis of a series of fused bicyclic s-[1,2,4]triazolo[1,5-a]pyridines 1 was accomplished utilizing novel intermediates derived from inexpensive, commercially available hydrazides A and methyl coumalate B. A significant fea
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e69d02cd4012d4ef081265407d3ae83c
https://pubmed.ncbi.nlm.nih.gov/28494588
https://pubmed.ncbi.nlm.nih.gov/28494588
Autor:
Prasad S. Raje, James P. Wepsiec, Nicholas A. Magnus, Chauncey D. Jones, Carlos Mateos, Amy C. DeBaillie, Alicia Torrado, Ramachandar Tokala
Publikováno v:
Organic Process Research & Development. 19:1568-1575
The development of a synthesis of an ORL-1 receptor antagonist is described. The key process improvements in the synthetic sequence include a multikilogram bromination process and the development of a convergent coupling strategy. The process improve
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2175ad9ed8acd4e92dc8b1978852dddf
https://doi.org/10.1021/op5000094
https://doi.org/10.1021/op5000094
Autor:
Sarah O’Keeffe, Rebecca E. Deasy, Humphrey A. Moynihan, Nicholas A. Magnus, Michael E. Kopach, Denis Lynch, Douglas Patton Kjell, David Mitchell, Orla A. McNamara, Catherine N. Slattery, Anita R. Maguire, Marie Kissane, Eric D. Moher
Publikováno v:
Organic Process Research & Development. 19:344-346
There is a growing trend in Ireland toward greater collaboration between academia and the pharmaceutical industry. This is an activity encouraged at a national policy level as a means of providing researchers from academic institutions the opportunit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5718c4f3e6551e8d0e5919e76f042488
https://doi.org/10.1021/op5003825
https://doi.org/10.1021/op5003825
Autor:
Gregory A. Stephenson, Bret A. Astleford, Dana L. T. Laird, John R. Rizzo, Adam D. McFarland, Todd D. Maloney, Nicholas A. Magnus, J. Craig Ruble, James P. Wepsiec
Publikováno v:
The Journal of Organic Chemistry. 78:5768-5774
Serotonin norepinephrine reuptake inhibitor (SNRI) pyrrolidinyl ether 2 was synthesized by employing a dynamic kinetic resolution (DKR) with enantio- and diastereoselective hydogenation on β-keto-γ-lactam 8 to afford β-hydroxy-γ-lactam 9 with 96%
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e081e825245116cbd0304abf9ef64731
https://doi.org/10.1021/jo400589j
https://doi.org/10.1021/jo400589j
Autor:
Amy C. DeBaillie, Michael A. Staszak, Michael E. Laurila, Nicholas A. Magnus, Chauncey D. Jones
Publikováno v:
Organic Process Research & Development. 17:231-238
An efficient and scalable process for the preparation of a purine-based CB2 agonist was developed. The production route to the requisite purine core relies on N-acylation and sequential substitution of a 5-amino-4,6-dichloropyrimidine with two amine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6f7e95e2c4bdb6a095149312fed45fd7
https://doi.org/10.1021/op300278c
https://doi.org/10.1021/op300278c
Autor:
Simon E. Lawrence, Nicholas A. Magnus, Catherine N. Slattery, Rebecca E. Deasy, Denis Lynch, Anita R. Maguire, U. B. Rao Khandavilli, Leslie-Ann Clarke, Humphrey A. Moynihan
Publikováno v:
Organic letters. 18(19)
Enantio- and diastereoselective hydrogenation of β-keto-γ-lactams with a ruthenium–BINAP catalyst, involving dynamic kinetic resolution, has been employed to provide a general, asymmetric approach to β-hydroxy-γ-lactams, a structural motif comm
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38cdcfd65df5374f10f15b1384e7489d
https://pubmed.ncbi.nlm.nih.gov/27656907
https://pubmed.ncbi.nlm.nih.gov/27656907
Autor:
Nicholas A. Magnus, Radhe K. Vaid, Jeffrey Petkus, James P. Wepsiec, Joseph F. Mick, Michael E. Laurila, Thomas Z. Gunter, J. Craig Ruble, Amy C. DeBaillie, Jeffry K. Niemeier
Publikováno v:
Organic Process Research & Development. 16:1538-1543
This contribution describes the demonstration of an asymmetric synthesis of a glucokinase activator via protonation of the enolate generated from an alkylaryl ketene and (R)-pantolactone. Additionally, a one-pot hydrolysis/oxidation protocol with lit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::976c62fbafdea6cc916f13f9b848aec0
https://doi.org/10.1021/op300139g
https://doi.org/10.1021/op300139g
Autor:
Jacob R. Remacle, Amy C. DeBaillie, Christopher P. Ley, Thomas Michael Wilson, Nicholas A. Magnus, Varie David Lee, Perry Clark Heath, Timothy M. Braden, Jonas Y. Buser
Publikováno v:
Organic Process Research & Development. 16:830-835
This article describes the development and optimization of chemical reactions and subsequent multikilogram preparation of the glucokinase activator (R)-1 to fund clinical evaluation as a potential therapeutic for type II diabetes. The major process d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c1fb7722475fb950612116d53a873c37
https://doi.org/10.1021/op300053a
https://doi.org/10.1021/op300053a
Autor:
James P. Wepsiec, D. Scott Coffey, Amy C. DeBaillie, Lin Wang, Iwona A. Kaluzna, Spiros Kambourakis, Nicholas A. Magnus, Chauncey D. Jones, Yangwei J. Pu
Publikováno v:
Organic Process Research & Development. 15:1377-1381
This communication describes proof of concept for an enantioselective enzyme-based synthesis of diarylmethanol (S)-1 to access mGlu2 receptor potentiators. A ketoreductase (KRED) screen was applied to benzophenone 8 to afford chiral diarylmethanol (S
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::607b8509d767e330d1083ce50e93e5c9
https://doi.org/10.1021/op2002479
https://doi.org/10.1021/op2002479