9/18/21 News Discover the magic of the 6-Butyltetrahydro-2H-pyran-2-one

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Chemistry is a science major with cience and engineering. The main research directions are chemical synthesis, new energy materials, preparation and modification of special coatings, and research on the structure and performance of functional materials3301-94-8, Name is 6-Butyltetrahydro-2H-pyran-2-one, molecular formula is C9H16O2. In a Article,once mentioned of 3301-94-8, Application of 3301-94-8

Replacing one amide bond in macrocyclic renin inhibitors of the general structure 1 and 2 with an ester linkage gave glutamate-derived inhibitors 3 and serine-derived inhibitors 4.While this oxygen-for-nitrogen exchange had little effect on potency in the glutamate series, potency was dramatically increased in the serine series.In this series, the 14-membered ring compounds proved to be more potent than the corresponding 13-membered ring derivatives.Substitution of the ring at the position corresponding to P2′ generally increased potency.The absolute configuration at this center was shown to be R for the 4-morpholinomethyl derivative (4o), both by asymmetric synthesis and X-ray crystallography.Replacing the “Boc-Phe” moiety of inhibitor 4o with a variety of substituents led to subnanomolar inhibitors, one of which (the “3(S)-quinuclidinyl-Phe” derivative 33) lowered blood pressure 20 mmHg and completely inhibited plasma renin activity for 6 h in sodium-depleted rhesus monkeys.This compound proved to have limited bioavailability (1 percent in rats) due to cleavage of the serine ester bond and rapid hepatic extraction.

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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics