Skip to Content
Merck
  • Synthesis of arylglycine and mandelic acid derivatives through carboxylations of α-amido and α-acetoxy stannanes with carbon dioxide.

Synthesis of arylglycine and mandelic acid derivatives through carboxylations of α-amido and α-acetoxy stannanes with carbon dioxide.

The Journal of organic chemistry (2012-02-01)
Tsuyoshi Mita, Masumi Sugawara, Hiroyuki Hasegawa, Yoshihiro Sato
ABSTRACT

Incorporation reactions of carbon dioxide (CO(2)) with N-Boc-α-amido and α-acetoxy stannanes were developed using CsF as a mild tin activator. Monoprotected α-amido stannanes could be used, and the corresponding arylglycine derivatives were obtained in moderate-to-high yields under 1 MPa (10 atm) of CO(2) pressure. α-Acetoxy stannanes also underwent carboxylation to afford mandelic acid derivatives in excellent yields under ambient CO(2) pressure. Both transformations enabled the synthesis of α-tertiary and α-quaternary carboxylic acid derivatives. In addition, the chirality of (S)-N-tert-butylsulfonyl-α-amido stannanes was transferred with up to 90% inversion of configuration at 100 °C.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Mandelic acid, 99%
Sigma-Aldrich
(R)-(−)-Mandelic acid, ReagentPlus®, ≥99%
Sigma-Aldrich
(R)-(−)-Mandelic acid, 98%
Sigma-Aldrich
(R)-(−)-Mandelic acid, ChiPros®, produced by BASF, 99%
Sertraline impurity E, European Pharmacopoeia (EP) Reference Standard
Supelco
DL-Mandelic acid, analytical standard