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HRID 1058828作成日:2026年10月23日
HCID 12721445、化合物 → 4-{(3-({1-[Bis-(4-chlorophenyl)methyl]azetidin-3-ylidene}methanesulfonylmethyl)benzoylamino]methyl}cyclohexanecarboxylic acid methyl ester
https://huagongshe.com/ja/reaction/1058828
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
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| 反応物 | HCID 12721445 | HCID 12721445 | — |
| 反応物 | 3-({1-[Bis(4-chlorophenyl)methyl]azetidin-3-ylidene}methanesulfonylmethyl)benzoic acid | HCID 69635678 | — |
| 溶媒 | Triethylamine | HCID 8471 | — |
| 生成物 | 4-{(3-({1-[Bis-(4-chlorophenyl)methyl]azetidin-3-ylidene}methanesulfonylmethyl)benzoylamino]methyl}cyclohexanecarboxylic acid methyl ester | HCID 69635613 | 38.2% |
反応手順
The operation is carried out under the conditions described in Example 124 starting with 110 mg of activated 3-({1-[bis(4-chlorophenyl)methyl]azetidin-3-ylidene}methanesulfonylmethyl)benzoic acid on TFP resin (121 μM), 0.026 cm3 of triethylamine and 39 mg of 4-aminomethylcyclohexanecarboxylic acid methyl ester hydrochloride. 47 mg of 4-{[3-({1-[bis-(4-chlorophenyl)methyl]azetidin-3-ylidene}methanesulfonylmethyl)benzoylamino]methyl}cyclohexanecarboxylic acid methyl ester are thus obtained in the form of a pale yellow paste [1H NMR spectrum (400 MHz, (CD3)2SO-d6, δ in ppm): from 0.90 to 1.05 (mt, 2H), from 1.20 to 1.40 (mt, 2H), 1.52 (mt, 1H), from 1.70 to 2.00 (mt, 4H), 2.27 (mt, 1H), 2.98 (s, 3H), 3.12 (t, J=6.5 Hz, 2H), 3.60 (s, 3H), 3.80 (mt, 2H), 4.23 (mt, 2H), 4.79 (s, 1H), 7.36 (d, J=8 Hz, 4H), 7.46 (d, J=8 Hz, 4H), from 7.45 to 7.60 (mt, 2H), 7.83 (broad s, 1H), 7.87 (broad d, J=8 Hz, 1H), 8.50 (t, J=6 Hz, 1H)].
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US06518264B2 |
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| 出典データセット | uspto-grants-2003_02 |
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| ORD ID | ord-707b9008805a425dbdee172d38b948ca |
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| 出典メモ | uspto-grants-2003_02 |
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