Use of an antibacterial agent for the treatment of an epithelial-related condition
一种用途、病况的技术，应用在抗细菌剂用于治疗上皮相关病况的用途领域
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example 1
[0354]
[0355] (4-((R)-1-carboxy-2-((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienylthio)ethylamino)- Synthesis of 4-oxobutanoic acid) (Compound B): To a solution of S-trans,trans-farnesyl-L-cysteine (500 mg, 1.54 mmol) in THF was added the first copies of K 2 CO 3 (2 mmol) and the resulting solution was cooled to 5°C while stirring vigorously. To this stirred solution was added succinic anhydride (308 mg, 3.1 mmol) dropwise while utilizing another portion of K 2 CO 3 (4 mmol) to maintain the pH at 9.0-10.0. The mixture was stirred at room temperature for 2 h, HPLC analysis showed the reaction was complete. The pH of the reaction mixture was then adjusted to 2.0 by adding 2N HCl solution. The acidic solution was extracted 3 times with 10 mL of ethyl acetate. The combined organic extracts were washed with water, brine and washed with Na 2 SO 4 Drying and removal of solvent on a rotary evaporator afforded crude compound B, which was further purified by preparative HP...
example 2
[0357]
[0358] ((E)-4-((R)-1-carboxy-2-((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienylthio)ethyl Synthesis of S-trans,trans-farnesyl-L-cysteine (500mg, 1.54mmol) in THF and the first part of K 2 CO 3 (3 mmol) was cooled to 5°C. To this stirred solution was added maleic anhydride (302mg, 3.07mmol) portionwise while utilizing another portion of K 2 CO 3 (3 mmol) to maintain the pH at 9.0-10.0. The mixture was stirred at room temperature for 3 h, HPLC analysis showed the reaction was complete. The pH of the reaction mixture was then adjusted to 2.0 by adding 2N HCl solution. The acidic solution was extracted 3 times with 15 mL of ethyl acetate. The combined organic extracts were washed with water, brine and washed with Na 2 SO 4 Drying and then concentration afforded crude Compound A, which was further purified by preparative HPLC (552 mg, 85%) to yield Compound A. 1 H-NMR (500MHz, CD 3 OD): δ1.50 (bs, 6H), 1.57 (s, 3H), 1.59 (s, 3H), 1.85-2.10 (m, 8H), 2.68 (dd, ...
example 3
[0360]
[0361] ((R)-2-((S)-2-Acetamido-3-hydroxypropionylamino)-3-((2E,6E)-3,7,11-trimethyldodeca-2,6, 10-trienylthio)propionic acid) and ((R)-2-((R)-2-acetylamino-3-hydroxypropionylamino)-3-((2E,6E)-3,7, 11-Trimethyldodeca-2,6,10-trienylthio)propionic acid)) Synthesis of a mixture (compound D): In a 100 mL round bottom flask, N-acetyl-L-serine ( 1.0mmol), coupling reagent (520mgPBOP or 380mgHATU, 1mmol) and N, N-diisopropyl-ethylamine (650mg, 5mmol) were mixed in CH 2 Cl 2 (10mL). The reaction mixture was stirred at room temperature for 30 minutes. S-trans,trans-farnesyl-L-cysteine (325 mg, 1 mmol) was added to the reaction mixture and stirred overnight at room temperature. CH removal by rotary evaporation 2 Cl 2 . The resulting residue was dissolved in ethyl acetate (50 mL). use NH 4 Cl saturated solution (50mL) washed the organic solution, washed with Na 2 SO 4 Dried and concentrated to obtain a crude mixture. The crude mixture was purified by preparative ...
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