CAS: 13838-08-9; 2-Azido-N-[(1R,2R)-1,3-Dihydroxy-1-(4-Nitrophenyl)Propan-2-Yl]Acetamide

上下游产品

azidoacetonitrile (1R,2R)-2-Amino-1-(4-nitrophenyl)-1,3-propanediol 2-azido-acetamide 2-azidoacetyl chloride(2S,3R) 2-amino-1-(4-aminophenyl)-1,3-propanediol 2-amino-1-(4-nitrophenyl)propane-1,3-diol

📜N-((1R,2R)-1-(4-Aminophenyl)-1,3-Dihydroxypropan-2-yl)-2-Azidoacetamide置于乙二胺四乙酸,Oxone,碳酸氢钠,Sodium Hydroxide体系中,用 水,丙酮 用作溶剂,化学反应 0.03H,以64%的收率获得叠氮氯霉素
参考文献:氨苯尼考抗生素的催化合成选择性硝基羟醛方法:(-)-氯霉素,(-)-阿齐达芬尼,(+)-甲硫苯尼考和(+)-氟苯尼考的统一不对称合成的演变
标题:氨苯尼考抗生素的催化合成选择性硝基羟醛方法:(-)-氯霉素,(-)-阿齐达芬尼,(+)-甲硫苯尼考和(+)-氟苯尼考的统一不对称合成的演变
摘要:报告了基于关键催化顺选择性亨利反应高效和高非对映选择性和对映选择性合成 (-)-氯霉素,(-)-阿齐丹苯,(+)-噻吩苯胺和 (+)-氟苯尼考的统一策略. 首次探索了配体启用的铜 (II) 催化的硝基乙醇的芳醛亨利反应的立体化学,以形成具有挑战性的合成-2-氨基-1,3-二醇结构单元,具有具有出色立体控制的邻位立体中心.进行了多步连续流动操作以实现该家族的双酚类抗生素的有效不对称合成.
Doi:10.1021/acs.Joc.1C01124

专利信息

专利号:US-8017776-B2
优先权日:2003-07-15
标题 :Methods for synthesis of acyloxyalkyl compounds
发明人：BHAT LAXMINARAYAN; GALLOP MARK A
权利人:XENOPORT INC
摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

专利号:US-8143437-B2
优先权日:2002-02-19
标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
发明人：GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X
权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC
摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

专利号:US-10472663-B2
优先权日:2015-01-21
标 题:Procedure for the rapid determination of bacterial susceptibility to antibiotics that inhibit protein synthesis
发明人：FERNÃ?NDEZ GARCÃ?A JOSÉ LUIS; GOSÃ?LVEZ BERENGUER JAIME; BOU ARÉVALO GERMÃ?N; TAMAYO NOVAS MARIA; SANTISO BRANDARIZ REBECA; OTERO FARIÑA FÃ?TIMA MARÃ?A
权利人:ABM TECH LLC
摘要:The present invention relates to a method for the rapid evaluation of bacterial susceptibility or non-susceptibility of bacteria to antibiotics that inhibit protein synthesis. The rationale is to identify bacterial responses that depend or are influenced by protein synthesis. If this response is prevented or reduced by the antibiotic that inhibits the protein synthesis, the bacteria are susceptible to this antibiotic. Otherwise, if the response keeps similar despite the incubation with the antibiotic, the bacteria are not susceptible or resistant to this antibiotic. These responses could be determined at the DNA lev-el, cell wall level, morphological level or any other experimental approach, including metabolic, bio-chemical, physiological or genetic processes.

专利号:US-2005070715-A1
优先权日:2003-07-15
标 题:Methods for synthesis of acyloxyalkyl compounds

专利号:US-7560483-B2
优先权日:2002-02-19
标题 :Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof

专利号:US-7662987-B2
优先权日:2003-07-15
标题:Methods for synthesis of acyloxyalkyl compounds