4-(4-chlorophenyl)-4-hydroxypiperidine
N-(dihydro-3,3-diphenyl-2(3H)-furanylidene)-N-methylmethanaminium bromide
loperamide hydrochloride
Conditions | Yield |
---|---|
Stage #1: 4-(4-chlorophenyl)-4-hydroxypiperidine With sodium carbonate; potassium iodide In 1,3-dioxolane-4-methanol for 0.25h; Stage #2: N-(dihydro-3,3-diphenyl-2(3H)-furanylidene)-N-methylmethanaminium bromide In 1,3-dioxolane-4-methanol at 60℃; for 2h; Stage #3: With hydrogenchloride In 1,3-dioxolane-4-methanol; isopropyl alcohol for 0.333333h; | 67% |
4-(4-chlorophenyl)-4-hydroxypiperidine
N-(dihydro-3,3-diphenyl-2(3H)-furanylidene)-N-methylmethanaminium bromide
4-methyl-2-pentanone
loperamide hydrochloride
Conditions | Yield |
---|---|
With potassium iodide; sodium carbonate In hydrogenchloride; isopropyl alcohol; acetone; toluene |
loperamide hydrochloride
methyl iodide
Conditions | Yield |
---|---|
With tetra-(n-butyl)ammonium iodide; sodium hydroxide In dichloromethane; water at 20℃; Inert atmosphere; | A 14% B 44% |
1. | orl-cld TDLo:125 µg/kg | BMJOAE British Medical Journal. 294 (1987),1383. | ||
2. | orl-rat LD50:185 mg/kg | JMCMAR Journal of Medicinal Chemistry. 16 (1973),782. | ||
3. | scu-rat LD50:78,700 µg/kg | NIIRDN “Drugs in Japan. Ethical Drugs, 6th Edition 1982“ Edited by Japan Pharmaceutical Information Center. 6 (1982),913. | ||
4. | ivn-rat LD50:7490 µg/kg | NIIRDN “Drugs in Japan. Ethical Drugs, 6th Edition 1982“ Edited by Japan Pharmaceutical Information Center. 6 (1982),913. | ||
5. | orl-mus LD50:105 mg/kg | ARZNAD Arzneimittel-Forschung. Drug Research. 24 (1974),1633. | ||
6. | ipr-mus LD50:28 mg/kg | ARZNAD Arzneimittel-Forschung. Drug Research. 24 (1974),1633. | ||
7. | scu-mus LD50:75 mg/kg | ARZNAD Arzneimittel-Forschung. Drug Research. 24 (1974),1636. | ||
8. | ivn-mus LD50:12,600 µg/kg | NIIRDN “Drugs in Japan. Ethical Drugs, 6th Edition 1982“ Edited by Japan Pharmaceutical Information Center. 6 (1982),913. | ||
9. | orl-gpg LD50:41,500 µg/kg | IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. 12 (1981),1204. |
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