Molecular Formula | C23H30O6S |
Molar Mass | 434.55 |
Density | 1.278±0.06 g/cm3(Predicted) |
Melting Point | 155.0-157.0℃ |
Boling Point | 624.5±55.0 °C(Predicted) |
pKa | 13.25±0.70(Predicted) |
hypoglycemic drug | Rugliejing is a SGLT-2 inhibitor type 2 diabetes treatment drug developed by Taisho Pharmaceutical Co., Ltd., formerly known as TS-071, by inhibiting SGLT2 reduces the reabsorption of renal filtered glucose and reduces the renal glucose threshold (RTG) in the urine to increase the excretion of urinary glucose. |
SGLT-2 inhibitor | In 2013, the United States approved the first SGLT-2 inhibitor hypoglycemic drug canagliflozin (Canagliflozin), which was developed by Johnson & Johnson. [mechanism of action] SGLT-2(type 2 Sodium Glucose co-Transportersinhibitor,SGLT2) is a transmembrane protein, which is mainly distributed in the proximal tubules of the kidney and transports glucose from renal tubular fluid into renal tubular cells, accounting for about 90% of the renal reabsorption of glucose. SGLT-2 inhibitors promote urine glucose excretion by inhibiting renal glucose reabsorption, moving the balance in the direction of energy expenditure, thereby reducing blood sugar in the body, and there is no risk of weight gain and hypoglycemia. It is a new type of drug for the treatment of diabetes. [adverse reactions] the most common adverse reactions of SGLT2 inhibitor drugs are the increased probability of urinary tract infection in patients taking drugs. If patients use Canagliflozin, the incidence of urinary tract infection increases, especially in female patients with type 2 diabetes, the incidence of vaginal candida infection increases. [listed drugs] the first half of 2014 was a half year of bumper harvest of SGLT2 inhibitor hypoglycemic drugs. In January 2014, the U.S. FDA approved the launch of the diabetes drug dagliflozin (Dapagliflozin), a SGLT-2 inhibitor, through Bristol-Myers Squibb/AstraZeneca. This is the second SGLT-2 inhibitor hypoglycemic drug approved by FDA. In addition, in 2014, the European Union approved the listing of a SGLT-2 inhibitor hypoglycemic drug Dapagliflozin/metformin compound dosage form, and Japan approved the listing of three SGLT-2 inhibitor hypoglycemic drugs, namely Togliflozin (Tofogliflozin), Aigliflozin (pragliflozin) and Lugliflozin (Luseogliflozin). |
refining method | in the first step, 13.6g of ruglerijing crude product is dissolved in 100ml of isopropanol-n-hexane mixed solvent; The volume ratio of isopropanol-n-hexane in the mixed solvent is 5:1; In the second step, at room temperature, 1.1g of activated carbon is added to the filtrate of the first step, stirred for 1 hour, and filtered. In the third step, the filtrate of the second step is cooled to 0 ℃ and kept unchanged, 5ml of 50% isopropanol aqueous solution is slowly added dropwise, and the speed of dropwise addition of 50% isopropanol solution is 0.70ml/min; White solid is precipitated, stirring is continued for 4-6 hours, and the stirring speed is 140 r/min minutes; In the fourth step, the filter cake is washed with 50% isopropanol solution for 3 times with a dosage of 8ml each time. In the fifth step, the filter cake is spread out and dried under vacuum at 40 ℃. |