Search results for "Allyl bromide"

showing 4 items of 4 documents

Synthesis of (E)- and (Z)-29-methylidyne-2,3-oxidosqualene derivatives as inhibitors of liver and yeast oxidosqualene cyclase

2002

The synthesis of (E)- and (Z)-29-methylidyne-2,3-oxidosqualene derivatives is described starting from the C22 and C17 squalene aldehyde monobromohydrins. The conversion was achieved by means of a Wittig reaction, followed by desilylation of the terminal acetylene. For trisubstituted 1,3-enynes, preliminary alkylation with a suitable allyl bromide was performed. A new procedure for the synthesis of squalene aldehyde C27, C22 and C17 monobromohydrins is also described. Some of the new compounds behaved as inhibitors of pig liver and yeast oxidosqualene cyclase and were time-dependent inhibitors of the animal enzyme.

chemistry.chemical_classificationAllyl bromideoxidosqualene derivatives; oxidosqualene cyclase; squaleneStereochemistryAlkylationsqualeneAldehydeYeast23-Oxidosqualenechemistry.chemical_compoundSqualeneEnzymechemistryWittig reactionoxidosqualene cyclaselipids (amino acids peptides and proteins)oxidosqualene derivatives
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ChemInform Abstract: Synthesis of (E)- and (Z)-29-Methylidyne-2,3-oxidosqualene Derivatives as Inhibitors of Liver and Yeast Oxidosqualene Cyclase.

2010

The synthesis of (E)- and (Z)-29-methylidyne-2,3-oxidosqualene derivatives is described starting from the C22 and C17 squalene aldehyde monobromohydrins. The conversion was achieved by means of a Wittig reaction, followed by desilylation of the terminal acetylene. For trisubstituted 1,3-enynes, preliminary alkylation with a suitable allyl bromide was performed. A new procedure for the synthesis of squalene aldehyde C27, C22 and C17 monobromohydrins is also described. Some of the new compounds behaved as inhibitors of pig liver and yeast oxidosqualene cyclase and were time-dependent inhibitors of the animal enzyme.

chemistry.chemical_classificationAllyl bromideStereochemistryGeneral MedicineAlkylationAldehydeYeast23-Oxidosqualenechemistry.chemical_compoundSqualeneEnzymechemistryWittig reactionlipids (amino acids peptides and proteins)ChemInform
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The Allyl Ester as Carboxy-Protecting Group in the Stereoselective Construction of Neuraminic-Acid Glycosides

1988

The application of the allyl-ester moiety as protecting principle for the carboxy group of N-acetylneuraminic acid is described. Peracetylated allyl neuraminate 2 is synthesized by reacting the caesium salt of the acid 1 with allyl bromide. Treatment of 2 with HCl in AcCl or with HF/pyridine gives the corresponding 2-chloro or 2-fluoro derivatives 3 and 4, respectively (Scheme 1). In the presence of Ag2CO3, the 2-chloro carbohydrate 3 reacts with di-O-isopropylidene-protected galactose 5 to give the 2–6 linked disaccharide with the α-D-anomer 6a predominating (α-D/β-D = 6:1; Scheme 2). Upon activation of the 2-fluoro derivative 4 with BF3 · Et2O, the β-D-anomer 6b is formed preferentially (…

Allyl bromideStereochemistryOrganic ChemistryDisaccharideBiochemistryCatalysisInorganic Chemistrychemistry.chemical_compoundchemistryNucleophileMorpholineDrug DiscoveryPyridineNeuraminic acidMoietyPhysical and Theoretical ChemistryProtecting groupHelvetica Chimica Acta
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ChemInform Abstract: The Allyl Ester as Carboxy-Protecting Group in the Stereoselective Construction of Neuraminic Acid Glycosides.

1989

The application of the allyl-ester moiety as protecting principle for the carboxy group of N-acetylneuraminic acid is described. Peracetylated allyl neuraminate 2 is synthesized by reacting the caesium salt of the acid 1 with allyl bromide. Treatment of 2 with HCl in AcCl or with HF/pyridine gives the corresponding 2-chloro or 2-fluoro derivatives 3 and 4, respectively (Scheme 1). In the presence of Ag2CO3, the 2-chloro carbohydrate 3 reacts with di-O-isopropylidene-protected galactose 5 to give the 2–6 linked disaccharide with the α-D-anomer 6a predominating (α-D/β-D = 6:1; Scheme 2). Upon activation of the 2-fluoro derivative 4 with BF3 · Et2O, the β-D-anomer 6b is formed preferentially (…

chemistry.chemical_compoundAllyl bromideNucleophilechemistryMorpholinePyridineNeuraminic acidDisaccharideMoietyGeneral MedicineProtecting groupMedicinal chemistryChemInform
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