Key Points：Difficulty of purification, Separation of Rectification, Cost-challenge, Industrial ton-production, High-Quality Requirement.
Applications: Key Building-Block for EGFR-inhibitor, etc: Osimertinib, Almonertinib, TAK-788
| Characteristics | Result |
|---|---|
| Boiling Point | 108 - 112°/ 760mmHgAzeotropy with water |
| Material Activity | reactive with halogenated Solvents, Ester Solvents. |
| Impurities Spectrum | Similarly Substituted-Amine |
| Water Solubiltiy | Easily soluble, mutually, |
Key Points：Cost-challenge, Industrial 10 tons-production per year, High-Quality Requirement 99.5%
Applications: Novel Salen Ligand Complex Catalyst Building-Block Downstream Compounds
| Characteristics | Result |
|---|---|
| Boiling Point | 110 - 112°/ 25mmHg |
| Material Activity | Light Sensitity & Metal Sensitity |
| Water Solubiltiy | Strong-Acidity, High-COD & NH3-Nitrogen |
Industrial Optimistic Process of HCV Ledipasvir Intermediates Key Points：Cost-challenge, Impurities-Limitation Challenge
Optimism of Process Parameters
Project Transfer Problem: Efficiency decreasing, Key-Impurties over the limits.
| Parameters | Lab Parameters | Scale-up Parameters |
|---|---|---|
| SM-A:SM-B: BASE | 1.2/1.0/1.1 | 0.9/1.0/0.95 |
| Solvent | THF or MTBE or Me-THF | THF |
|
Feeding Sequence SM-A:SM-B: BASE |
SM-B and Base with dropping SM-A Solution |
SM-B and Base but feeding with SM-A in solid |
| SM Forma | N.A. | SM-A Crystalline Form |
| Temperature | -30°- R.T. | -15°- R.T. |
| Type of Stirring | Magnetic Stirring | Anchor |
| Purification | Recrystrallation & Column | Recrystrallation |
| Deviation of Effienciey | 64%-75% Efficiency | 70% - 80% |
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