A highly efficient synthesis of telaprevir by strategic use of biocatalysis and multicomponent reactions.

نویسندگان

  • Anass Znabet
  • Marloes M Polak
  • Elwin Janssen
  • Frans J J de Kanter
  • Nicholas J Turner
  • Romano V A Orru
  • Eelco Ruijter
چکیده

A very short and efficient synthesis of the important drug candidate telaprevir, featuring a biocatalytic desymmetrization and two multicomponent reactions as the key steps, is presented. The classical issue of lack of stereoselectivity in Ugi- and Passerini-type reactions is circumvented. The atom economic and convergent nature of the synthetic strategy require only very limited use of protective groups.

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

Deep Eutectic Solvent Based on Choline Chloride/Urea as an Efficient Catalytic System for the One-Pot Synthesis of Highly Functionalized 1,4-Dihydropyridines and Polysubstituted 4H-Chromenes

One-pot four-component synthesis of polyfunctionalized 1,4-dihydropyridine derivatives was developed by a condensation of aldehydes, malononitrile, diethylacetylenedicarboxylate and aniline in the presence of choline chloride/urea as a deep eutectic solvent (DES)at room temperature.Moreover, an efficient method was reported for the synthesis of highly substituted 4H-chromenes through one-...

متن کامل

Highly efficient and rapid synthesis of diverse hydantoin derivatives using nano-ordered ZnO catalyst under mechanochemical ball milling

A mild and efficient one-pot three-component and environmentally benign approach for the synthesis of a wide range of hydantoin annulated derivatives has been described. A multi-component reaction between a carbonyl compounds (ketone or aldehyde), potassium cyanide and ammonium carbonate (as cyanating agent and amine source, respectively leads to the formation of hydantoins. The proposed optimi...

متن کامل

Efficient Synthesis of Nickel(II) Complex Supported on Fe3O4@SiO2 Nanoparticles as a New and Facile Catalyst for Various Multicomponent Reactions

In the present work, we have planned a new magnetically recoverable nanocatalyst. The obtained nanocatalyst designated as Fe3O4@SiO2@DOPisatin-Ni (II) was characterized by FTIR, XRD, SEM, EDAX, VSM, AAS and TGA techniques. It was found that Fe3O4@SiO2@DOPisatin-Ni (II) successfully catalyses the synthesis of 2,3-dihydroquinazolin-4(1H)-ones, polyhydroquinoline and 5-substituted 1H-tetrazoles in...

متن کامل

Employing a hydrophobic-bentonite as a highly efficient and versatile catalyst for a green one-pot and rapid synthesis of 4H-benzo-[b]-pyran derivatives

A hydrophobic-bentonite catalyst (cetyltrimethyl ammonium bromide-bentonite) has been used as a very mild, neutral, eco-friendly, reusable, non-toxic, low-cost and easily available catalyst. It was prepared by replacing the exchangeable Na+ cations of a homoionic Na–bentonite with cetyltrimethyl ammonium bromide (CTMAB) cations. The catalyst was characterized by XRD, BET and SEM. The...

متن کامل

Employing a hydrophobic-bentonite as a highly efficient and versatile catalyst for a green one-pot and rapid synthesis of 4H-benzo-[b]-pyran derivatives

A hydrophobic-bentonite catalyst (cetyltrimethyl ammonium bromide-bentonite) has been used as a very mild, neutral, eco-friendly, reusable, non-toxic, low-cost and easily available catalyst. It was prepared by replacing the exchangeable Na+ cations of a homoionic Na–bentonite with cetyltrimethyl ammonium bromide (CTMAB) cations. The catalyst was characterized by XRD, BET and SEM. The...

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 communications

دوره 46 42  شماره 

صفحات  -

تاریخ انتشار 2010