Document Detail


Practical asymmetric synthesis of β-hydroxy γ-amino acids via complimentary aldol reactions.
MedLine Citation:
PMID:  21822337     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Orthogonally protected chiral β-hydroxy-γ-amino acids can be accessed in >100 g quantities from readily available starting materials and reagents in 3-4 steps. These chiral synthons contain two adjacent stereocenters along with suitably protected functional groups (O-TBS, N-Boc) for downstream reactivity. Implementation of two existing aldol technologies allows rapid access to all possible stereoisomers of 1. The guiding principles during reaction optimization were reaction scalability and operational efficiency. Conversion of the amino acids to a variety of chiral building blocks in 1-2 steps demonstrates their synthetic utility.
Authors:
Bhaumik A Pandya; Sivaraman Dandapani; Jeremy R Duvall; Ann Rowley; Carol A Mulrooney; Troy Ryba; Michael Dombrowski; Marie Harton; Damian W Young; Lisa A Marcaurelle
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Publication Detail:
Type:  JOURNAL ARTICLE    
Journal Detail:
Title:  Tetrahedron     Volume:  67     ISSN:  0040-4020     ISO Abbreviation:  -     Publication Date:  2011 Aug 
Date Detail:
Created Date:  2011-8-8     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  2984170R     Medline TA:  Tetrahedron     Country:  -    
Other Details:
Languages:  ENG     Pagination:  6131-6137     Citation Subset:  -    
Affiliation:
Chemical Biology Platform, The Broad Institute of MIT and Harvard, 7 Cambridge Center, Cambridge, MA 02142, USA.
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Descriptor/Qualifier:
Grant Support
ID/Acronym/Agency:
P50 GM069721-11//NIGMS NIH HHS; RL1 HG004671-05//NHGRI NIH HHS

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