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Synthetic Chemistry Case Studies

BACKGROUND:

Client requested synthesis of 3.5 kg novel compound with 98% purity with procedure suitable for scale-up

CHALLENGES:

Compound solubility in organic solvents was very low. Client’s internal procedure yield was low and not suitable for scale-up

RESULTS:

Designed a new route with a 4 step scale-up capability demonstrating a dramatically improved yield, compound was purified by re-crystallization, delivered in 5 weeks

BACKGROUND:

Client requested synthesis of 3 Kg with 98% purity and 98% e.e. of a novel chiral compound

CHALLENGES:

Client’s internal procedure yield was low due to byproduct formation requiring chiral SFC to yield pure enantiome0, high cost made it not suitable for scale-up

RESULTS:

Designed new synthetic route yielding >99% e.e. by chiral reduction and re-crystallization, delivered in 9 weeks

BACKGROUND:

Client requested synthesis of  9 kg with 98% purity and 98% e.e. of a novel chiral compound under GLP

CHALLENGES:

Client’s route was 12 steps requiring preparative HPLC and Chiral SPC separation, requiring large amounts of m-CPBA, NaN3, and LAH. Complexity and reagent cost made it not suitable for scale-up

RESULTS:

Designed a new synthetic route with 6 steps and good chiral purity without HLPC, and SFC separation requiring no m-CPBA, NaN3, and LAH, delivered in 13 weeks