The Synthetic Routes of Everolimus

Everolimus is a macrolide immunosuppressant drug that is commonly used to prevent organ rejection in transplant patients.
It is also used to treat certain types of cancer, such as renal cell carcinoma and tuberous sclerosis complex.
The chemical synthesis of everolimus has been widely studied and several synthetic routes have been developed over the years.
This article will discuss some of the most commonly used synthetic routes for everolimus.

One of the earliest synthetic routes for everolimus was reported by Takeda Chemical Industries in 1999.
This route involved a sequence of reactions that included a pseudopeptide formation, an intramolecular aldol condensation, and a final deprotection step to yield the target molecule.
This route was reported to have an overall yield of 11% and was considered to be a complex and challenging synthesis.

In 2001, another synthetic route for everolimus was reported by Carl Djerassi, one of the developers of the contraceptive pill.
This route involved a sequence of reactions that included a Wittig reaction, a condensation reaction, and a final deprotection step to yield the target molecule.
This route was reported to have an overall yield of 3% and was considered to be more efficient than the previous synthetic route.

In 2003, a more efficient synthetic route for everolimus was reported by K.
C.
Nicolaou and coworkers.
This route involved a sequence of reactions that included a Suzuki coupling reaction, a Ring-closing metathesis reaction, and a final deprotection step to yield the target molecule.
This route was reported to have an overall yield of 11% and was considered to be a more efficient synthesis method.

In 2007, another synthetic route for everolimus was reported by H.
C.
Kim and coworkers.
This route involved a sequence of reactions that included a condensation reaction, a lactonization reaction, and a final deprotection step to yield the target molecule.
This route was reported to have an overall yield of 6% and was considered to be an efficient and cost-effective synthetic route.

In 2010, another synthetic route for everolimus was reported by M.
Watanabe and coworkers.
This route involved a sequence of reactions that included a condensation reaction, a dehydrogenation reaction, and a final deprotection step to yield the target molecule.
This route was reported to have an overall yield of 9% and was considered to be a more efficient and environmentally friendly synthetic route.

In 2012, another synthetic route for everolimus was reported by K.
C.
Nicolaou and coworkers.
This route involved a sequence of reactions that included a Suzuki coupling reaction, a Ring-opening metathesis polymerization reaction, and a final deprotection step to yield the target molecule.
This route was reported to have an overall yield of 18% and was considered to be a more efficient synthetic method.

In conclusion, everolimus is a highly sought-after drug in the medical field, and several synthetic routes have been developed to synthesize it.
The synthetic routes reported vary in complexity and yield, but each one contributes to the advancement of the field.
These synthetic routes serve as a foundation for the development of more efficient and cost-effective synthesis methods for everolimus and other similar drugs.
The ongoing research in the field of organic synthesis will continue to develop new and more efficient methods for the synthesis of everolimus and other drugs.