Green preparation technology has experienced two stages, one is from the traditional craft to asymmetric catalytic hydrogenation stage, the second is asymmetry catalytic hydrogenation process to metal phase.
The green pharmaceutical form of the drug is a biological enzyme preparation technology.
in 2006 the FDA approved a diabetes, is a 4 second skin base skin enzyme (
D PP -
This drug by protecting endogenous im fall blood sugar, and enhance its role and control blood sugar.
In 2012, sales of 40.
900 million dollars.
Its production technology is to use a successful example of asymmetric catalytic hydrogenation, and green pharmaceutical good case.
Original process using multi-step reactions to the preparation of the API, including the introduction of the group of protection and protection, and quantitatively using chiral amine, these will inevitably increase the reagent type and dosage of solvent, is contrary to the principles of green chemistry.
in the study of synthesis process, successfully abandoned as the introduction of the chiral amine of auxiliary reagent and chiral induction, the catalysts, chiral mountain ligands and reaction conditions such as solvent, temperature, pressure, reaction time and other process variables after investigation found that bare enamine does not require phthalein, can be directly in asymmetric catalytic hydrogenation and selectively preparation high optical activity of amino phthalein amine, ee value as high as 98%, and successfully implemented the industrialized production asymmetric catalytic hydrogenation preparation of chiral drugs than traditional split method is a lot of green environmental protection, but also is not perfect, there are still a series of problems and defects.
In order to overcome these problems and defects, Merck and other researchers studied greener enzyme technology will intermediate step into 20 chiral amine, and amine donor for isopropyl amine, generated by-products for acetone.
In the west he dean enzyme preparation process.
the place on put together is narrated, the rise of green pharmaceutical technology is the disappearance of chemical pharmaceutical, both to reduce the chemical pharmaceutical pollution to the environment, to achieve the ecological environment protection, and to a certain extent, promoted the progress and development of modern pharmaceutical industry, increase the height of the modern pharmaceutical industry, for the sustainable development of the modern pharmaceutical technology has laid a solid foundation.
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