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Example 87A (S)-N-Boc-2-Formyl-pyrrolidine STR115 (S)-N-Boc-2-Formyl-pyrrolidine was prepared by Swern oxidation of (S)-N-Boc prolinol (Fluka) according to the conditions described by M. G. B. Drew et al., J. Chem. Soc. Perkin 1, 1998, 1627, for the oxidation of CBZ-prolinol.
With ammonium acetate; In dimethyl sulfoxide; at 60℃; for 2h;
The compound DSV102 (2.63g) and dimethyl sulfoxide (30ml) were added to a 50ml three-necked flask, and reacted at 30 C for 31 hours.Ammonium acetate (2.31 g), L-Boc guanaldehyde (1.99 g), and reacted at 60 C for 2 h. Add 30ml of anhydrous methanol dropwise, stir at 25 CAt night (14h), suction filtration, solid washing with water (20ml * 3), drying at 80 C under vacuum, to obtain 2.81g solid DSV01, yield 90%,The purity is 96%.
With ammonium acetate; In dimethyl sulfoxide; at 30℃; for 4h;
Add to a 100ml two-neck bottleBrominated biphenyl diacetyl(1.98g),Dimethyl sulfoxide (20ml),The reaction was carried out at 25 C for 16 h, and ammonium acetate (2.31 g) was added.L-Boc-prolinal(1.99 g), reacted at 30 C for 4 h.Add 20 ml of anhydrous methanol, 20 ml of water, and stir for 45 min.Filter by suction, wash the solid with water (20ml * 3), vacuum dry at 80 C,Obtained 2.66 g of solid DSV01,The yield is 85%,The purity is 94%.
Add DSV101 (1.54g) to a 50ml three-necked flask,Potassium bromide (0.30 g), dimethyl sulfoxide (10 ml),After reacting at 75 C for 6 h, the temperature was lowered, and ammonium acetate (2.31 g) was added.L-Boc guanylaldehyde (1.99 g) was reacted at 40 C for 5 h. Add 100ml of water,The organic layer was washed with brine (100 ml)Separation by column chromatography2.56g solid DSV01,The yield is 82%.The purity is 95%
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