New One-Pot Synthesis of ò-Iodoalkyne

A high yielding, one-pot general procedure for the synthesis of ò-iodoalkyne is described.     

One-Pot Synthesis of Pyrazolyl-Containing α-Aminophosphonates

Abstract

A series of novel pyrazolyl-containing α-aminophosphonates were synthesized by one-pot reaction from 4-formylpyrazole, substituted aromatic amines, and dialkylphosphites. The synthesized compounds were characterized by elemental analysis, ¹H NMR, and IR spectroscopy. Single-crystal X-ray diffraction data of compounds 4a and 5b were obtained, and some of these compounds showed inhibitory effect on eggplant-infecting Botrytis cinerea.

Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements for the following free supplemental resource: Tables S1-S4. Figures S1 and S2 .cif files.     

Convenient Solid-phase Synthesis of Benzothiazole Derivatives

Resin-bound cyclic malonic ester 1 reacted with aryl isothiocynate, then was treated with bromine, followed by cleavage from the resin under perchloric acid to give benzothiazoles 4.     

Convenient Synthesis of N-Benzyl-N′-acyl-piperazines

The importance of N,N′ asymmetrically disubstituted piperazines in pharmaceutical and medicinal chemistry does not need to be emphasized. Such a basic moiety is present in a number of drugs belonging to different classes, and especially in those of the central and peripheral nervous system. In recent times the interest connected with piperazines appears to be a fast growing topic in drug research.     

A Convenient Synthesis of β-Ketosulfoxides

β-Ketosulfoxideshaveattractedmanyorganicchemistsbecauseoftheirwideuseinsynthesisofketones,a-ketols,glyoxals,a-ketoacids,glycols,a-hydroxyacidsandsoculGenerally,6-ketosulfoxidescanbepreparedbythereactionofesterwithsulfoxidel',acylchloridewithsulfoxi...     

A New Convenient Synthesis of Pyridine-N-oxides

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Novel and Convenient Approach to Synthesis of AZT／d4T H-phosphonates

A convenient, efficient and general method has been developed for synthesis of H-phosphonate mono and diesters of AZT and d4T through one-pot reaction of phosphonic acid with AZT or d4T and different alcohols using pivaloyl chloride as condensing agent under mild conditions.     

A Convenient Method of Synthesis of Ferrocenylethynyl Ketones

It is well known that molecules possessing extensive conjugated π-electron systems exhibit large non-linear optical properties,[1,2] but the compounds of ferrocenylethynyl ketones have not been reported so far. We now reported preparation of some ferrocenylethyl ketones. These new ethynylketones containing ferrocenyl were prepared conveniently via coupling reaction catalyzed by PdCl2(PPh3)2/PdBzCl(PPh3)2-CuI from ferrocenylethyne and acyl chlorides. This coupling reaction proceeded smoothly in argon and free-water atmosphere at room temperature and gave coupling products in satisfactory yields. All products were characterized by 1H NMR, MS, IR and UV spectra.     

A Convenient Synthesis of ω-Acetylenic Acids

ω-Acetylenic acids are valuable intermediates in the synthesis of long-chain acids. Their dimagnesium salts may be alkylated with 1-bromo-2-alkynes or 2-alkenes to synthesize many important naturally occurring fatty acids^1–3. Also, internally-monounsaturated acids are prepared by alkylation of ω-acetylenic acid dilithium salts^4,5 or the sodium salts of their N,N-dimethylamides⁶.     

Convenient Synthesis of 3,5‐Disubstituted Isoxazoles

α,β‐Unsaturated oximes obtained from the corresponding α,β‐unsaturated ketones on treatment with 2 equivalents of manganese dioxide in refluxing chloroform gives 3,5‐disubstituted isoxazoles in good yields.     

A Convenient Synthesis of Protected α-Hydroxyacetaldehydes

Starting from 2, 3-O-isopropylideneglycerol (1), a general procedure for the preparation of protected α-hydroxyacetaldehydes has been developed.     

Convenient Synthesis of 5‐Aryl Uracils

A convenient one‐step synthesis of 5‐aryl uracils has been developed. The procedure involves heating ethyl 3‐hydroxy‐2‐arylpropenate with urea at 130°C, followed by base‐catalyzed cyclization. The method is simple and high yielding.     

A Convenient Synthesis of β-Amino Acid

We have reported the reductive cleavage of azlactones¹ and phenylhydrazones² of carbonyl compounds in the presence of a suitable catalyst. In this paper a general method involving a one step synthesis of β-amino acid^3,4, in good yield, through catalytic reduction of oximes of α-β-unsaturated acid is reported. This method involves the reaction of α, β-unsaturated acid with hydroxylamine hydrochloride in the presence of sodium acetate. Markovnikov's rule is followed in the synthesis of oximes of α, β-unsaturated acids.     

Convenient One-Pot Synthesis of β-Alkylthio Acid Derivatives from Thioacetates and the Corresponding α,β-Unsaturated Compounds

Various β-alkylthio acid derivatives were prepared conveniently from thioacetates and α,β-unsaturated compounds through borohydride exchange resin (BER)-Pd catalyzed transesterification of thioacetates to the corresponding thiols and Michael addition of the resulting thiols to α,β-unsaturated compounds.     

Synthesis of β-Amino Phosphonates in One-Pot Procedure

Abstract: β-amino phosphonate derivatives are synthesized in one-pot procedure via reduction of β-enamino phosphonate intermediates with NaBH₄/acetic acid or trifluoroacetic acid.     

Facile and Efficient One-Pot Synthesis of β-Carbolines

Initial formation of tetrahydrocarboline 3 from tryptophan methyl ester 1 and aldehyde 2 by Pictet–Spengler reaction, followed by treatment with trichlorocyanuric acid, provides a facile and efficient route for a one-pot synthesis of β-carbolines with excellent yields.     

Synthesis of β-Lactams by Convenient Annelation of Imines

2-Acyl-3-oxo-4,5-benzo-1,2-thiazoline 1,1-dioxide (3) provides good yield routes to monocyclic 3-lactams (6) and tricyclic β-lactams (7) from a variety of imines (4) and 1-substituted-3,4-dihydroisoquinolines (5).     

Convenient Synthesis of Uridine 5′ - Oxyphosphorane

Uridine 5′-oxyphosphorane was synthesized by the reaction of 2′, 3′-di-O-acteyluridine 5′-diisopropyl phosphite with tetrachloro-1, 2-benzoquinone.     

A Convenient Synthesis of α-Hydrosyiminoacetonitriles from Aldoximes

Aromatic α-hydroxyiminoacetonitriles can be conveniently prepared by a facile one-pot procedure in high yields involving chlorination of the corresponding aldoximes with tert-butyl hypochlorite followed by reaction with alkali cyanide.     

A Convenient Synthesis of α-Hydroxyiminoacetonitriles From Aldoximes

Aromatic α-hydroxyiminoacetonitriles can be conveniently prepared by a facile one-pot procedure in high yields involving chlorination of the corresponding aldoximes with tert-butyl hypochlorite followed by reaction with alkali cyanide.