JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
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129.8, 127.9, 114.5, 73.0, 70.9, 33.8, 23.9, 21.6, 18.1, 18.1, 12.3. [a]20 -7.2 (c 0.27,
D
MeOH); HRESIMS: m/z 427.2328 [M þ H]þ (calcd for C22H40O4SSi, 427.2333).
3.2.6. (R)-6-(1H-Pyrrol-1-yl)hex-1-en-3-ol (5)
Pyrrole (0.017 mL, 0.24 mmol) was added to a stirred suspension of NaH (10 mg,
0.24 mmol) in dry N, N-dimethylformamide (1 mL), and the resulting solution was
starred at room temperature for 5 min. Then, a solution of tosylate (51.8 mg,
0.12 mmol) in DMF (0.5 mL) was added, and the flask containing the tosylate was
rinsed with additional DMF (0.2 mL). The resulting mixture was stirred at room tem-
perature for 2 h, and then, a solution of TBAF (0.5 mL, 0.5 mmol, 1 M in THF) was
added and stirred at room temperature overnight. The reaction mixture was
quenched with water, and the aqueous layer was extracted with ethyl acetate. The
combined organic extracts were washed with brine, dried over Na2SO4, filtered, and
concentrated in vacuo. Purification by flash column chromatography (PE/EtOAc ¼
4:1) gave title compound (18.6 mg, 93%) as a colorless oil. 1H NMR (600 MHz,
CDCl3) d 6.66 (s, 2H), 6.14 (s, 2H), 5.84 (ddd, J¼ 17.2, 10.4, 6.2 Hz, 1H), 5.22 (d,
J¼ 17.2 Hz, 1H), 5.12 (d, J¼ 10.4 Hz, 1H), 4.09 (q, J¼ 6.2 Hz, 1H), 3.91 (tt, J¼ 8.5,
4.2 Hz, 2H), 1.99–1.76 (m, 2H), 1.54–1.49 (m, 2H). 13C NMR (151 MHz, CDCl3) d
140.8, 120.5, 115.1, 107.9, 72.8, 49.5, 33.9, 27.4. [a]20 -2.5 (c 0.12, MeOH);
D
HRESIMS: m/z 166.1221 [M þ H]þ (calcd for C10H16NO, 166.1226).
3.2.7. Methyl (R, E)-4-hydroxy-7-(1H-pyrrol-1-yl) hept-2-enoate (8)
To a solution of the alcohol (0.26 g, 1.6 mmol) in DCM (4 mL) were added methyl
acrylate (1.4 g, 16 mmol) and the Grubbs second generation catalyst (66 mg,
0.082 mmol) at room temperature in sealed tube. The deep brown reaction mixture
was raised to 40 ꢀC and stirred for 24 h. The reaction mixture was concentrated to
afford residue, which was purified by column chromatography (hexane: EtOAc ¼
4:1) to afford the desired product (0.32 g) as brown oil (Yield: 92%). 1H NMR
(600 MHz, CDCl3) d 6.92 (dd, J¼ 15.7, 4.9 Hz, 1H), 6.66 (s, 2H), 6.16 (t, J¼ 2.1 Hz,
2H), 6.05 (dd, J¼ 15.7, 1.7 Hz, 1H), 4.34–4.25 (m, 1H), 3.97–3.88 (m, 2H), 3.77 (s,
3H), 1.98–1.81 (m, 2H), 1.54–1.62 (d, 2H). 13C NMR (126 MHz, CDCl3) d 166.9,
150.0, 120.5, 120.1, 108.1, 70.5, 51.7, 49.3, 33.5, 27.2. [a]20 -3.4 (c 0.27, MeOH).
D
3.2.8. (3aR, 10bR)-1, 3a, 4, 5, 6, 10b-Hexahydro-2H-furo[3, 2-c]pyrrolo[1, 2-a]aze-
pin-2-one (19). To a solution of ester (25 mg, 0.11 mmol) in DCM (3.8 mL) was
added the boron trifluoride diethyl etherate (0.017 ml, 0.14 mmol) at 0 ꢀC. The reac-
tion mixture was warmed to room temperature and stirred overnight. Triethylamine
was added to the reaction mixture and stirred for 30 min. The organic layer was
washed with H2O and concentrated to afford residue, which was purified by column
chromatography (PE: EtOAc ¼ 4:1) to afford the desired product 19 (9.6 mg) as
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white solid (Yield: 57%). H NMR (600 MHz, CDCl3) d 6.70–6.59 (m, 1H), 6.05 (dd,
J¼ 3.4, 2.8 Hz, 1H), 5.99–5.92 (m, 1H), 4.14 (dd, J¼ 14.6, 5.4 Hz, 1H), 4.00 (ddd,
J¼ 11.2, 10.1, 3.5 Hz, 1H), 3.91 (dd, J¼ 14.2, 11.8 Hz, 1H), 3.43 (dd, J¼ 15.4, 6.0 Hz,
1H), 2.98–2.87 (m, 2H), 2.60–2.50 (m, 1H), 2.20–2.10 (m, 1H), 1.88–1.80 (m, 1H),