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15th December 2011 @ 05:40
**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 MNR12-1

Reducing reaction time and temperature of MW54-3

MNR12-1%20scheme.png

MNR12-1%20table.PNG

Hazard and Risk Assessment:
As for MNR12-2

Procedure
MNR8-2 (120 mg, 0.26 mmol) was stirred with methanesulfonic acid (1.7 mL, 26 mmol) at room temperature and after 1 hours (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 - 112 mgs as an orange oil that slowly crystallised over the weekend.

1H NMR MNR12-1-crude

Lab book page complete, MNR
Attached Files
mnr12-1_crude.zip
mnr12-1_crude.pdf
kab8-16.zip
kab8-16 1H 500.pdf
kab8-16 13C 500.pdf