Case Histories:

1) A Client requested a twenty fold scale-up of their procedure which reported a 75% product yield with 25% starting material contamination. The Client deemed any purification too costly at this stage and, hence, the crude material was used in their next step, with a concomitant drop in expected yield.

Solution: A front-run was done to familiarize and corroborate the client’s procedure prior to the twenty-fold material commitment. Information gained from this run suggested modification of the procedure maybe beneficial. Incorporating these modifications, another front-run confirmed the evaluation.
The reaction condition modifications increased the yield to 95% with no starting material contamination. Applying a more fitting isolation protocol, a crystalline product of 99% purity was obtained and delivered. Use in the Client’s next reaction step now met yield expectations. Total R&D effort: 2 days. 

2)  A client requested a regioselectively protected (BOC) diamine.
A standard orthogonal protection/de-protection strategy was un-successful, as the product proved highly solution sensitive to BOC trans-migration to the more basic amine.

Solution: Employing a new synthetic strategy, a route was developed providing the protected amine in high yield (97%), before the latent unprotected amine was unmasked under conditions compatible with the BOC stability. The crystalline product was isolated in 85% yield of >98% purity.
Total R&D effort:      3 weeks


3)  A client supplied procedure produced variable (10-30%) yield material of poor purity after extractive isolation. Exacting chromatographic purification only exacerbated the yield. A simple scale-up would not meet the customers timely, material needs.

Solution: The monitored reaction indicated a good conversion positing product decomposition upon extractive isolation. Conditions were developed to crystallize the product directly from the reaction solution, affording an un-optimized 89% isolated yield of 99% purity, suitable to scale-up.
Total R&D effort : 2 weeks

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