Synthesis Of Dapagliflozin, Canagliflozin And Their Analogues

Diabetes is one of ‘the three diseases’ in the 21 st century that seriously threatens people’s health and safety, the study of anti-diabetic drugs have become the focus of the medical field. SGLT-2 is an important glucose transporter protein that responsible for sugar re-absorption in the kidney.Studies have shown that inhibition of SGLT-2activity may specifically inhibit the re-absorption of glucose, thus excreted the excess sugar. It can be effective in the treatment of type Ⅱ diabetes, and no serious side effects caused by traditional medicines.As a new target of anti-type Ⅱ diabetes, the research progress of SGLT-2inhibitors is rapid. Till now, Dapagliflozin and Canagliflozin have been listed in the foreign market for the treatment of type Ⅱ diabetes. In this paper, it contains the synthesis of Dapagliflozin and Canagliflozin by two different methods of glucose modification which are bromo-glucose protected by Piv and glucose lactone protected by Benzyl. Then it compares the relative advantages and disadvantages of the two routes from the ease of operation, cost, product yield, etc. Another important part of this paper is the design and synthesis of structurally similar compounds by structure-activity relationship analysis. This paper can be reference for the research of more pharmaceutical value SGLT-2 Inhibitors.