An efficient and concise access to 2-amino-4H-benzothiopyran-4-one derivatives

• Peng Li,
• Yongqi Wu,
• Tingting Zhang,
• Chen Ma,
• Ziyun Lin,
• Gang Li and
• Haihong Huang

Beilstein J. Org. Chem. 2019, 15, 703–709, doi:10.3762/bjoc.15.65

• Chinese Academy of Medical Sciences, 1 Xian Nong Tan Street, Beijing 100050, P. R. China 10.3762/bjoc.15.65 Abstract A highly efficient and convenient protocol was developed to access 2-amino-4H-benzothiopyran-4-ones through a process of conjugated addition–elimination. The sulfinyl group was proved to

• good yields and excellent chemical purity without requiring column chromatographical purification. Keywords: 2-amino-4H-benzothiopyran-4-ones; addition–elimination; scale-up synthesis; sulfinyl group; Introduction Benzothiopyranones are a class of molecules displaying biological activities in part

• or sulfonyl moiety with higher reactivity at the 2-position of the benzothiopyranone ring. In our continuing efforts to discover novel 2-amino-4H-benzothiopyran-4-ones with activity against Mycobacterium tuberculosis (Mtb) [5], we aim to develop an improved and efficient synthetic route by thoroughly