Composition and method for scalp and hair treatment
A hair treatment and composition technology, applied in the field of hair and scalp treatment, can solve the problems of insufficient blood circulation nutrition, defective waste excretion function and the like
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Embodiment 1
[0101] 13,14-Dihydro-15,15-trimethylenedioxy-20-ethyl-PGF 2α Isopropyl ester (5)
[0102]
[0103] To a solution of compound 1 (510.0 mg, 1.273 mmol) in toluene (10.2 ml) was added 1,3-propanediol (0.92 ml, 12.73 mmol) and a catalytic amount of p-toluenesulfonic acid and the mixture was heated under reflux 17 hours. Thereafter, the reaction was kept standing until it cooled to room temperature, washed with saturated aqueous sodium bicarbonate and sodium chloride aqueous solutions. The organic phase was dried over magnesium sulfate and evaporated under reduced pressure. The residue was purified by silica gel column chromatography (Merck 7734, hexane:ethyl acetate=3:2) to obtain compound 2 (581.3 mg).
[0104] A solution of compound 2 (580.0 mg, 1.265 mmol) in toluene (11.6 ml) was cooled to -78 °C, 1.5M-DIBAH (in toluene, 2.95 ml, 4.427 mmol) was added dropwise thereto and the mixture was stirred for 1 hours, methanol (1.79 ml) was then added dropwise to the resulting mixt...
Embodiment 2
[0110] 13,14-dihydro-15,15-dimethoxy-20-ethyl-PGF 2α Isopropyl ester (10)
[0111]
[0112] To a solution of compound 1 (797.8 mg, 2.002 mmol) in methanol (2.4 ml) was added catalytic amounts of p-toluene sulfate, methyl orthoformate (2.19 ml, 20.02 mmol) and anhydrous magnesium sulfate (1.20 g, 10.01 mmol) And heated to reflux for 4 hours. The reaction was cooled and sodium bicarbonate was added, and filtered using celite. The filtrate was evaporated under reduced pressure and the residue was purified by silica gel column chromatography (Merck 7734g, hexane:ethyl acetate=3:2) to obtain compound 7 (884.3 mg, yield 98.9%).
[0113] compound 7 (767.5mg, 1.719mmol) in toluene (15.4ml) was cooled to -78°C, 1.5M-DIBAH (in toluene, 4.0ml, 6.016mmol) was added dropwise thereto and the mixture was stirred for 1 hour. Methanol was then added dropwise to the reaction and the reaction was allowed to warm to room temperature. Saturated aqueous Rochelle's salt solution (150 ml) wa...
Embodiment 3
[0119] 13,14-Dihydro-15,15-ethylenedioxy-17-phenyl-18,19,20-trinor-PGF 2α Isopropyl ester (12)
[0120] In the same manner as in the synthetic examples, the compound 11 Preparation of compounds 12 .
[0121]
[0122] compound 11 of 1 H-NMR spectrum (200MHz, CDCl 3 ): δ 8.04-7.93 (2H, m), 7.63-7.38 (3H, m), 7.35-7.11 (5H, m), 5.21-5.03 (2H, m), 2.98-2.24 (HH, m), 2.12- 1.98(1H,m), 1.80-1.50(2H,m)
[0123] compound 12 of 1 H-NMR spectrum (200MHz, CDCl 3 ): δ7.35-7.12 (5H, m), 5.56-5.35 (2H, m), 5.00 (1H, sept, J=6.2Hz), 4.15 (1H, bs), 3.96 (4H, s), 3.92 ( 1H, bs), 3.18 (1H, bd), 2.86 (1H, bd), 2.75-2.63 (2H, m), 2.28 (2H, t, J=7.3Hz), 2.46-1.15 (17H, m), 1.22 (6H, d, J=6.2Hz)
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