Furo(3,2-b)indole derivatives. III Structure-activity studies of 4,6-disubstituted N-(3-piperidinopropyl)furo(3,2-b)indole-2-carboxamide derivatives for analgesic and antiinflammatory activities.

Kawashima, Y.; Sato, Masakazu; Hatada, Y.; Okuyama, Shigeru; Amanuma, Fusao; Nakashima, Y.; Sota, Kaoru; Moriguchi, Ikuo

doi:10.1248/cpb.34.3267

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“…Synthetic compounds with the structural motif of furo[3,2‐ b ]indoles are of vital medicinal value 1. They show pronounced pharmacological effects such as anti‐allergy,1a potent analgesic1b–e,2 anti‐inflammatory1b,d–i and anti‐pyretic activities 1d,j. Not only that, they are also key intermediates for the synthesis of several natural products 3.…”

Section: Methodsmentioning

confidence: 99%

Microwave‐Assisted Facile Synthesis of Furo[3,2‐b]indole Derivatives via Silver(I)‐Mediated [3+2] Cycloaddition

Zhang¹,

Fang²,

Li³

et al. 2012

Adv Synth Catal

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A robust one-pot process has been developed for the synthesis of a variety of furoA, Ag 2 O (0.058 g, 0.25 mmol) and KOH (0.028 g, 0.5 mmol) was well stirred for 1.5 h under microwaves in CH 3 CN (3.0 mL), then to the mixture was added water (10 mL) and HCl (0.5 M, 1 mL), followed by extraction with CH 2 Cl 2 (15 mL 3). The solvent was removed under reduced pressure, and the residue was purified by a short flash silica gel column chromatography (eluent: diethyl ether/petroleum ether = 1/2) to give compound 2b; yield: 0.084 g (76%).

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