Delving into the Latest Updates on Bervastatin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

HMG-CoA reductase

Mechanism

HMG-CoA reductase inhibitors(HMG-CoA reductase inhibitors)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication-

Inactive Indication

Hypercholesterolemia

Originator Organization

Merck Serono SA

Active Organization-

Inactive Organization

Merck Serono SA

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC28H31FO5

InChIKeyZADJRRFMOOACHL-FFOZXMBFSA-N

CAS Registry132017-01-7

AbstractWe have developed a general and site‐predictable manganese‐catalyzed hydroarylation of internal alkynes in the presence of water, under an air atmosphere without the involvement of ligand. The unique catalytic feature of this reaction is highlighted by comparison with other widely used transition metal catalysts including palladium, rhodium, nickel, or copper. The simple operation, high efficiency and excellent functional group compatibility make this protocol practical for more than 90 structurally diverse internal alkynes, overcoming the influence of both electronic and steric effect of alkynes. Its exclusive regio‐ and chemoselectivity originates from the unique reactivity of the manganese‐based catalyst towards an inherent double controlled strategy of sterically hindered propargyl alcohols without the installing of external directing groups. Its synthetic robustness and practicality have been illustrated by the concise synthesis of bervastatin, a hypolipidemic drug, and late‐stage modification of complex alkynes with precise regioselectivity.

100 Deals associated with Bervastatin

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