Molecular Formula | C36H47N5O4 |
Molar Mass | 613.79 |
Density | 1.25±0.1 g/cm3(Predicted) |
Melting Point | 153-154°; mp 167.5-168° |
Boling Point | 877.9±65.0 °C(Predicted) |
Specific Rotation(α) | D22 +24.1° (c = 0.0133 in chloroform) |
Flash Point | 484.731°C |
Water Solubility | 70mg/L(temperature not stated) |
Vapor Presure | 0mmHg at 25°C |
pKa | pKa 3.8/6.2(H2O,t undefined,Iundefined) (Uncertain) |
Storage Condition | 2-8℃ |
Refractive Index | 1.636 |
Physical and Chemical Properties | Monohydrate: crystallized from wet ethyl acetate or isopropyl acetate. Water loss below 100 ° C., recrystallization to obtain anhydrous, the melting point of 153-154 ° C.; The second anhydrous melting point of 167.5 ~ 168C. Solubility in water (mg/ml):0.015 (no buffer),>1.5(pH = 4.0). [Α] D22 24.1. (C = 0.0133, chloroform). Indinavr sulfate: C36Ha7N5O4? H2SO4. [157810-81-6]. It appears as a monoethanolic compound. Crystallization from anhydrous ethanol, softening point of 135 deg C, melting point of 150~153 deg C (decomposition). Loss of ethanol or exposure to moisture to form hydrates. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.629 ml | 8.146 ml | 16.292 ml |
5 mM | 0.326 ml | 1.629 ml | 3.258 ml |
10 mM | 0.163 ml | 0.815 ml | 1.629 ml |
5 mM | 0.033 ml | 0.163 ml | 0.326 ml |
biological activity | Indinavir(MK-639; L735524) is an HIV protease inhibitor with good oral biocompatibility. |
use | antiviral drugs. It is a novel hydroxyaminopentane amide HIV-1 protease inhibitor used to treat AIDS. |
production method | at -50 ℃, the weak base Lithium hexamethyl disilazide(LHS) is added to the solution of compound (I) and (S)-(+)-dehydrated glycerol toluenesulfonate (II), then the temperature is increased to -25 ℃, and the compound (III) with 72% yield is obtained by reaction. (Ⅲ) and compound (Ⅳ) are refluxed in isopropanol (IPA), and then 6mol/L hydrochloric acid is added to remove the protective group on N to obtain compound (V). Finally, it reacts with 3-pyridinecarboxylic chloride to obtain the product. The yield is 71% based on compound (III). |