3,4-二氢-1-(4-哌啶基)-2(1H)-喹啉酮的合成

以苄胺为原料,经6步反应得到新型抗高血压药OPC-21268的中间体3,4-二氢-1-(4-哌啶基)-2(1H)-喹啉酮,总收率13．9％．     

A Convenient Synthesis of N-Substituted 1,6-Dihydro-3(2H)-Pyridinones

N-Substituted 1,6-dihydro-3(2H)-pyridinones have been synthesised from N-substituted piperidine-3,5-diones via the methyl enol ethers. Reduction of the latter with sodium borohydride (NaBH₄) is described.     

5-羟基-3,4-二氢异喹啉-1-酮的合成

以异喹啉为起始原料,经成盐、磺化得异喹啉-5-磺酸(3),3与熔融的氢氧化钠和氢氧化钾反应得1,5-二羟基异喹啉(4),以5%Pd-C为催化剂还原4得5-羟基-3,4-二氢异喹啉-1-酮(1),总收率47.6%。1的结构经1H NMR和MS确证。     

A Convenient Synthesis of 2-Aryl-3-per(poly)fluoroacylindoles

ＩｎｔｒｏｄｕｃｔｉｏｎＤｕｅｔｏｔｈｅｓｐｅｃｉｆｉｃｐｒｏｐｅｒｔｉｅｓｉｍｐａｒｔｅｄｂｙｆｌｕｏｒｉｎｅ ,ｔｈｅｉｎｔｒｏｄｕｃｔｉｏｎｏｆａｆｌｕｏｒｉｎｅａｔｏｍｏｒａｆｌｕｏｒｏａｌｋｙｌｇｒｏｕｐｉｎｔｏｌｅａｄｍｏｌｅｃｕｌｅｓｈａｓｂｅｅｎｗｉｄｅｌｙｕｓｅｄａｓｏｎｅｏｆｔｈｅｍｅｔｈｏｄｓｆｏｒｔｈｅｄｅｖｅｌｏｐｍｅｎｔｏｆｎｏｖｅｌｂｉｏｌｏｇｉｃａｌｌｙａｃｔｉｖｅｃｏｍｐｏｕｎｄｓ.1Ｉｎｄｏｌｅｓａｒｅａｔｔｒａｃｔｉｖｅｃｏｍｐｏｕｎｄｓｆｒｏｍｔｈｅｖｉｅｗｐ…     

Synthesis of 1(2H)-Isoquinolones. (Review)

Methods published over the last 10 years for the production of substituted 1(2H)-isoquinolones, including those involving the use of organometallic compounds, are discussed.     

A Convenient Synthesis Of 2-Methyl-5-(Methylthio)Benzothiazole

A convenient and efficient four step synthesis of 2-methyl-5-(methylthio)benzothiazole is presented.     

An Efficient Synthesis of 3,4-Dihydro-4-Imino-2(1H)-Quinazolinones

A new one-pot convenient preparation of 3,4-dihydro-4-imino-2(1H)-quinazolinones (4) is described by the reaction of 2-aminobenzonitriles (1) with chlorosulfonyl isocyanate (2), while the reaction of 1 with chlorocarbonyl isocyanate (6) affords ureidobenzonitriles (7), which on thermal cyclization gives 4.     

2-甲基-6-(3-甲基-2-丁烯基)对苯二醌的合成

以邻甲基苯酚为原料,与1-氯-2-甲基-2-丁烯反应生成2-甲基-6-(3-甲基-2-丁烯基)苯酚,然后催化氧化得到目标产物2-甲基-6-(3-甲基-2-丁烯基)对苯二醌。该合成路线简单,易于操作,最终收率51%。     

Convenient Synthesis of 5-Aryl-1-(1H-pyrazol-4-yl)pyrrolidin-2-ones

Russian Journal of Organic Chemistry - Heating of 4-aryl-N-(1H-pyrazol-4-yl)but-3-enamides in polyphosphoric acid selectively afforded 5-aryl-1-(1H-pyrazol-4-yl)pyrrolidin-2-ones.     

Synthesis of 4-Oxo-1,2,3,4-tetrahydropyridine (2,3-Dihydro-4(1H)pyridinone)

N-Ethoxycarbonyl-4-pyridone is reduced to N-ethoxycarbonyl-4-oxo-1, 2, 3, 4-tetrahydropyridine by sodium borohydride in t-butyl alcohol containing ethyl chloroformate. Saponification of the product leads to 4-Oxo-1, 2, 3, 4-tetrahydropyridine.     

A Convenient Synthesis of 3-Aryl-3-(5,5-dimethyl-3-hydroxy-2-cyclohexene-1-one-2-yl) Propanic Esters Catalyzed by KF-Alumina

A series of 3-aryl-3-(5,5-dimethyl-3-hydroxy-2-cyclohexene-1-one-2-yl) propanic esters were synthesized by reaction of aromatic aldehydes, 5,5-dimethyl-1,3-cyclohexanedione and isopropylidene malonate in alcohols catalyzed by KF-Al₂O₃. The structure of 4a was determined by X-ray analysis.     

Chemoselective Dehydrogenation of 3-[2-（3,4-Dihydro-1-naphthalenyl）ethyl]imidazolidine-2,4-diones： a New and Convenient Synthesis of 13,16-Diazaequilenin analogs

The synthesis of the title compounds starting with the chemoselective dehydrogenation of 3-[2-(3,4-dihydro-1-naphthalenyl)ethyl]imidazolidine-2,4-diones has been described.     

2-芳基-3,4-二氮杂芴酮和2-芳基-3,4-二氮杂螺二芴衍生物的合成

水合茚三酮与芳甲基酮、水合肼缩合环化制得2-芳基-3,4-二氮杂芴酮(2); 2经还原得2-芳基-3,4-二氮杂芴(3).2与2-溴联苯格氏试剂反应得到中间体叔醇(4); 4在酸性条件下关环合成了2-芳基-3,4-二氮杂螺二芴,其结构经1H NMR,13C NMR和元素分析表征.     

A Novel Synthesis of 3,4-Dihydro-(2H)-1,2,4-Benzothiadiaizine-1,1-Dioxides Promoted by Samarium Diiodide

Applicationsofsamariumdiiodideasamild,neutral,selectiveandversatilesingleelectrontransferreducingandcouplingreagentinorganicsynthesishavesignificantlygrowninthelastdecade'.PreviousworkonsomedeoxygenationandsomereductivecleavageofS-S,Se-Se,Te-TebondswithSml,wasreported'.ItiswellknownthatnitrocompoundscanbereducedeasilybySml2.However,theyarejustreducedtothecorrespondingammes',lit'tleattentionhasbeenconcernedontheintermediatederivedfromanitrogroupbySml,treatment,whichmaybeinducesomereactionsd…     

Facile Synthesis of 6-Aryl-3-cyanopyridine-2-(1H)-thiones from Aryl Ketones

An improved synthesis of 6-aryl-3-cyanopyridine-2-(1H)-thiones utilizing enaminones as starting materials catalyzed by 1,4-diazabicyclo[2.2.2]octane (DABCO) was described. Moreover, a convenient one-pot conversion of aryl ketones to 6-aryl-3-cyanopyridine-2-(1H)-thiones was also developed in moderate to good yields (up to 80%).     

A Useful Synthesis of 3-Methyl-2(5H)-Furanone

An efficient procedure for the preparation of furanone 3 from commercially available starting material lactone 1, is reported.