N
Neal W. Sach
Researcher at Pfizer
Publications - 57
Citations - 3385
Neal W. Sach is an academic researcher from Pfizer. The author has contributed to research in topics: Aryl & Anaplastic lymphoma kinase. The author has an hindex of 22, co-authored 54 publications receiving 2632 citations. Previous affiliations of Neal W. Sach include Scripps Research Institute.
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Journal ArticleDOI
Practical and innate carbon–hydrogen functionalization of heterocycles
Yuta Fujiwara,Janice A. Dixon,Fionn O’Hara,Erik Daa Funder,Darryl D. Dixon,Rodrigo A. Rodriguez,Ryan D. Baxter,Bart Herlé,Neal W. Sach,Neal W. Sach,Michael R. Collins,Michael R. Collins,Yoshihiro Ishihara,Phil S. Baran +13 more
TL;DR: It is reported that zinc sulphinate salts can be used to transfer alkyl radicals to heterocycles, allowing for the mild, operationally simple formation of medicinally relevant C–C bonds while reacting in a complementary fashion to other innate C–H functionalization methods.
Journal ArticleDOI
Discovery of (10R)-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and c-ros Oncogene 1 (ROS1) with Preclinical Brain Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations
Ted William Johnson,Paul F. Richardson,Simon Bailey,Alexei Brooun,Benjamin J. Burke,Michael R. Collins,J. Jean Cui,Deal Judith G,Ya-Li Deng,Dac M. Dinh,Lars D. Engstrom,Mingying He,Jacqui Elizabeth Hoffman,Robert Louis Hoffman,Qinhua Huang,Robert Steven Kania,John Charles Kath,Hieu Lam,Justine L. Lam,Phuong Le,Laura Lingardo,Wei Liu,Michele McTigue,Cynthia Louise Palmer,Neal W. Sach,Tod Smeal,Graham L. Smith,A.E. Stewart,Sergei Timofeevski,Huichun Zhu,Jinjiang Zhu,Helen Y. Zou,Martin Paul Edwards +32 more
TL;DR: This work led to the discovery of 8k (PF-06463922), combining broad-spectrum potency, central nervous system ADME, and a high degree of kinase selectivity, which was found to be potent against wild-type ALK and clinically reported ALK kinase domain mutations.
Journal ArticleDOI
Strain Release Amination
Ryan Gianatassio,Justin M. Lopchuk,Jie Wang,Chung-Mao Pan,Lara R. Malins,Liher Prieto,Thomas Andrew Brandt,Michael R. Collins,Gary M. Gallego,Neal W. Sach,Jillian E. Spangler,Huichin Zhu,Jinjiang Zhu,Phil S. Baran +13 more
TL;DR: A general strategy to harness the embedded potential energy of effectively spring-loaded C–C and C–N bonds with the most oft-encountered nucleophiles in pharmaceutical chemistry, amines is reported.
Journal ArticleDOI
A platform for automated nanomole-scale reaction screening and micromole-scale synthesis in flow.
Damith Perera,Joseph W. Tucker,Shalini Brahmbhatt,Christopher John Helal,Ashley Chong,William Farrell,Paul G. Richardson,Neal W. Sach +7 more
TL;DR: An automated flow-based synthesis platform that integrates both rapid nanomoles-scale reaction screening and micromole-scale synthesis into a single modular unit is reported here.
Journal ArticleDOI
Electrochemically Driven, Ni-Catalyzed Aryl Amination: Scope, Mechanism, and Applications
Yu Kawamata,Julien C. Vantourout,David P. Hickey,Peng Bai,Longrui Chen,Qinglong Hou,Wenhua Qiao,Koushik Barman,Martin A. Edwards,Alberto F. Garrido-Castro,Justine N. deGruyter,Hugh Nakamura,Kyle W. Knouse,Chuanguang Qin,Khalyd J. Clay,Denghui Bao,Chao Li,Jeremy T. Starr,Carmen N. Garcia-Irizarry,Neal W. Sach,Henry S. White,Matthew Neurock,Shelley D. Minteer,Phil S. Baran +23 more
TL;DR: Through a series of electrochemical, computational, kinetic, and empirical experiments, the key mechanistic features of this reaction have been unraveled, leading to a second generation set of conditions that is applicable to a broad range of aryl halides and amine nucleophiles.