Synthesis of the side chain of a novel carbapenem via iodine-mediated oxidative cyclization of (1R)-N-(1-aryl-3-butenyl)acetamide.

نویسندگان

  • Takashi Hashihayata
  • Hiroki Sakoh
  • Yasuhiro Goto
  • Koji Yamada
  • Hajime Morishima
چکیده

A (2R,4S)-trans-disubstituted pyrrolidine ring system was constructed by employing iodine-mediated oxidative cyclization of (1R)-N-[1-(4-bromophenyl)-3-butenyl]acetamide 3 as a key step. The resulting diastereomeric mixture of (2R)-2-aryl-4-acetoxypyrrolidine 4 was stereoselectively converted to the side-chain of a novel ultrabroad-spectrum carbapenem 1, via (2R,4R)-2-aryl-4-hydroxypyrrolidine 7.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Synthesis of some new 2-(3-aryl-1-phenyl-4-pyrazolyl)-benzoxazoles using hypervalent iodine mediated oxidative cyclization of Schiff's bases.

Ten new 2-(3-aryl-1-phenyl-4-pyrazolyl)benzoxazoles have been synthesized by oxidative intramolecular cyclization of the corresponding Schiff's bases using iodobenzene diacetate in methanol as an oxidant.

متن کامل

A facile iodine(III)-mediated synthesis of 3-(3-aryl-1-phenyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridines via oxidation of 2-((3-aryl-1-phenyl-1H-pyrazol-4-yl)methylene)-1-(pyridin-2-yl)hydrazines and their antimicrobial evaluations

BACKGROUND Fused heterocyclic 1,2,4-triazoles have acquired much importance because of their interesting biological properties. Although a number of methods have been reported in the literature which includes oxidation with phosphorus oxychloride, lead tetraacetate, bromine, etc., hypervalent iodine reagents have emerged as reagents of choice for various synthetically useful transformations due...

متن کامل

Room temperature copper(II)-catalyzed oxidative cyclization of enamides to 2,5-disubstituted oxazoles via vinylic C-H functionalization.

A copper(II)-catalyzed oxidative cyclization of enamides to oxazoles via vinylic C-H bond functionalization at room temperature is described. Various 2,5-disubstituted oxazoles bearing aryl, vinyl, alkyl, and heteroaryl substituents could be synthesized in moderate to high yields. This reaction protocol is complementary to our previously reported iodine-mediated cyclization of enamides to affor...

متن کامل

Synthesis, Characterization and Study of Some N-Substituted Aryl-2- ({4-[(Substituted Aryl Carbamoyl) Methyl]-5-(Pyridin-4-yl)-4H-1, 2, 4-Triazol-3-yl} Sulfanyl) Acetamide

Pathogenic infections and inflammation are very common ailments humans suffer. Upsurge of resistant pathogens has impeded the antimicrobial drug development process in recent years and the search of new antimicrobial agents is clearly evident from the literature. In line with these developments the synthesis of N-substituted aryl-2-({4-[(substituted aryl carbamoyl) methyl]-5-(pyridin-4-yl)-4H-1...

متن کامل

Towards Synthesis of Atropodiastereomeric Indolostilbenes Hybrids: A New Class of Oligostilbenoids

The conceptually construction of axially chiral indolostilbenesi.eN-(2-{(E)-2-[2'-(1-Acetyl-1H-indol-2-yl)-3'chloro4,4',6,6'-tetramethoxy[1,1'-biphenyl]-2yl]ethenyl}phenyl)acetamide and N-(2-{(E)-2-[2'-(1-Acetyl-1H-indol-2-yl)-3'-chloro-2,4',6,6'tetramethoxy[1,1'-biphenyl]-4-yl]ethenyl}phenyl) acetamide are described in this paper. These structure, were obtained by the tactical combination of p...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Chemical & pharmaceutical bulletin

دوره 50 3  شماره 

صفحات  -

تاریخ انتشار 2002