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15th December 2011 @ 05:56
**I've been locked out of the previous post due to mix up in google accounts**

Acid-mediated Pictet-Spengler of MNR8-2 to give dimethoxy-N-benzoyl-derivative of PZQ MNR12-2

Repeat of MNR12-1 but at 60°C

MNR12-2%20scheme.png

MNR12-2%20table.PNG

Hazard and Risk Assessment:
HIRAC MNR12.pdf


Procedure:
MNR8-2 (130 mg, 0.28 mmol) was stirred with methanesulfonic acid (1.8 mL, 28 mmol) at 60°C and after 1 hour (first TLC) all the starting material had been consumed. The reaction was quenched with saturated sodium carbonate and extracted with EtOAc (20 mL x2). The organic fractions were dried over magnesium sulfate, filtered and concentrated under reduced pressure.

Crude - 72 mgs as an orange oil

1H NMR MNR12-2-crude

Lab book page complete, MNR
Attached Files
mnr12-2_crude.pdf
mnr12-2_crude.zip