其它产品项目整合

项目整合的本质是一项集合成方法学、反应工程学与过程分析技术于一体的系统工程。其核心逻辑可以概括为以下几点：源头优选：利用如N-硝胺化学等底层方法学突破，从分子层面颠覆传统高成本、高污染路线。过程强化：依托连续流技术，攻克有机金属试剂应用、光化学反应放大等“不可能”任务，实现高危工艺的本质安全。系统集成：整合“反应-淬灭-分离”全流程，利用微流控与在线分析技术，消除批次间的差异，实现药品制造的连续化与智能化。当前，中间体工艺研发正在经历从“经验驱动”向“数据驱动”的转变。AI辅助路线设计、自动化高通量筛选与连续制造平台的结合，将使得“分子结构与最优工艺路径”之间的映射关系逐渐清晰。未来的竞争优势，将属于那些能够将底层化学创新与先进工程技术进行无缝整合的研发体系。
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其它产品项目整合

Pivampicillin CAS Registry Number: 33817-20-8 匹凡西林

CAS Name: (2S,5R,6R)-6-[[(2R)-Aminophenylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid (2,2-dimethyl-1-oxopropoxy)methyl ester
Additional Names: hydroxyme...
Literature References: Semi-synthetic antibiotic related to penicillin. Prepn: E. K. Frederiksen, W. O. Godtfredsen, ZA 6805952; eidem, US 3660575 (1969, 1972 to Lövens Kemiske Fabrik); von Daehne et al., J. Med. Chem. 13, 607 (1970). Pharmacology: eidem, loc. cit.; Jordan et al., Antimicrob. Agents Chemother. 1970, 438; Foltz et al., ibid. 442. Pharmacokinetics in man: M. Ehrnebo et al., J. Pharmacokinet. Biopharm. 7, 429 (1979). Toxicity: von Daehne et al., Antimicrob. Agents Chemother. 1970, 430.

Nafcillin CAS Registry Number: 147-52-4 萘夫西林

CAS Name: (2S,5R,6R)-6-[[(2-Ethoxy-1-naphthalenyl)carbonyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Additional Names: 6-(2-ethoxy-1-naphthamido)penicillin Literature References: Semi-synthetic antibiotic related to penicillin. Prepn: F. P. Doyle et al., GB 880400; F. P. Doyle, J. H. C. Nayler, US 3157639 (1961, 1964 both to Beecham). Prepn of crystalline monohydrate: D. Flitter et al., US 3506645 (1970 to American Home Prod.). HPLC determn: P. Fan-Havard, M. C. Nahata, Ther. Drug Monit. 11, 105 (1989). Antibacterial activity: J. M. Steckelberg et al., Antimicrob. Agents Chemother. 37, 554 (1993). Clinical efficacy: D. L. Palmer et al., Ann. Thorac. Surg. 59, 626 (1995).

Talampicillin CAS Registry Number: 47747-56-8 酞氨西林

CAS Name: (2S,5R,6R)-6-[[(2R)-Aminophenylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid 1,3-dihydro-3-oxo-1-isobenzofuranyl ester
Additional Names: (2S,5R,...
Literature References: Semi-synthetic antibiotic related to penicillin. Prepn: H. Ferres, M. P. Clayton, DE 2228012; eidem, US 3860579 (1972, 1975 both to Beecham). See also: M. Murakami et al., US 3951954 (1976 to Yamanouchi). Pharmacology: Clayton et al., Antimicrob. Agents Chemother. 5, 670 (1974). HPLC determn in urine and comparison of pharmacokinetics with other aminopenicillins: T. Uno et al., Chem. Pharm. Bull. 29, 1957 (1981). Clinical comparison with ampicillin, q.v.: H. N. Williams et al., Br. J. Clin. Pract. 35, 147 (1981).

Dicloxacillin CAS Registry Number: 3116-76-5 双氯西林

CAS Name: (2S,5R,6R)-6-[[[3-(2,6-Dichlorophenyl)-5-methyl-4-isoxazolyl]carbonyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Additional Names: 6-[3-(2,6-dichlor...
Literature References: Semi-synthetic antibiotic related to penicillin. Prepn: J. H. C. Naylor, GB 978299; eidem, US 3239507 (1965, 1969 to Beecham). Toxicity data: C. Gloxhuber et al., Arzneim.-Forsch. 15, 322 (1965). Series of articles on chemistry, pharmacology and toxicology: ibid. 322-348; Matsuzaki, Jpn. J. Antibiot. 21, 274, 284 (1968), C.A. 70, 95267z, 95265x (1969).

Carindacillin CAS Registry Number: 35531-88-5 卡茚西林

CAS Name: (2S,5R,6R)-6-[[3-[(2,3-Dihydro-1H-inden-5-yl)oxy]-1,3-dioxo-2-phenylpropyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Additional Names: N-(2-carboxy...
Literature References: Semi-synthetic antibiotic related to penicillin. Prepn: K. Butler, ZA 6900060; idem, US 3679801 (1969, 1972 both to Pfizer). New process: S. Nakanishi, US 3759898 (1973 to Pfizer). Activity studies: Butler, Del. Med. J. 43, 366 (1971); English et al., Antimicrob. Agents Chemother. 1, 185 (1972). Clinical evaluation: Wallace et al., Antimicrob. Agents Chemother. 1970, 223; Bran et al., Clin. Pharmacol. Ther. 12, 525 (1971); Indanyl Carbenicillin, H. Swarz, F. E. Storari, Eds. (Am. Elsevier, New York, 1974) 100 pp.

Amoxicillin CAS Registry Number: 26787-78-0 阿莫西林

CAS Name: (2S,5R,6R)-6-[[(2R)-Amino(4-hydroxyphenyl)acetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Additional Names: (-)-6-[2-amino-2-(p-hydroxyphenyl)acet...
Literature References: Semi-synthetic antibiotic related to penicillin. Prepn: Nayler, Smith, GB 978178 (1964 to Beecham); eidem, US 3192198 (1965); Long, Nayler, DE 1942693 and GB 1241844 (1970 and 1971 to Beecham), C.A. 72, 90447q (1970). Resolution of isomers: Long et al., J. Chem. Soc. C 1971, 1920. Series of articles on activity, pharmacology, absorption and excretion: Antimicrob. Agents Chemother. 1970, 407-430. Review of antibacterial activity, pharmacokinetics and therapeutic use: R. N. Brogden et al., Drugs 18, 169-184 (1979). Comprehensive description: A. E. Bird, Anal. Profiles Drug Subs. Excip. 23, 1-52 (1994).

Sulbenicillin CAS Registry Number: 41744-40-5 磺苄西林

CAS Name: (2S,5R,6R)-3,3-Dimethyl-7-oxo-6-[[(2R)-phenylsulfoacetyl]amino]-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Additional Names: a-sulfobenzylpenicillin; sulfocillin
Percent C...
Literature References: Semi-synthetic antibiotic related to penicillin. Prepn: S. Morimoto et al., DE 1948943 corresp to US 3660379 (1970, 1972 both to Takeda); eidem, J. Med. Chem. 15, 1105, 1108 (1972). In vitro activity studies: Tsuchiya et al., J. Antibiot. 24, 607 (1971); in vivo: Yamazaki, Tsuchiya, ibid. 620. Metabolism: Tsuchiya et al., ibid. 25, 336 (1972). Toxicity: Y. Murata et al., Takeda Kenkyushoho 30, 262 (1971), C.A. 76, 147x (1972). Pharmacokinetics: A. Montanari et al., Clin. Ter. 89, 163 (1979); eidem, Int. J. Clin. Pharmacol. Ther. Toxicol. 18, 225 (1980).

Clometocillin CAS Registry Number: 1926-49-4 双氯甲氧青霉素

CAS Name: (2S,5R,6R)-6-[[(3,4-Dichlorophenyl)methoxyacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Additional Names: 3,4-dichloro-a-methoxybenzylpenicillin...
Literature References: Semi-synthetic antibiotic related to penicillin. Prepn: Vanderhaeghe et al., Antimicrob. Agents Chemother. 1961, 581; US 3007920 (1961 to Recherche et Ind. Therap.). Activity studies: van Dijck et al., Antibiot. Chemother. 12, 192 (1962).

Epicillin CAS Registry Number: 26774-90-3 依匹西林

CAS Name: (2S,5R,6R)-6-[[(2R)-Amino-1,4-cyclohexadien-1-ylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Additional Names: 6-[D-a-amino-2-(1,4-cyclohexadie...
Literature References: Semi-synthetic antibiotic related to penicillin. Prepn: Weisenborn et al., US 3485819 (1969 to Squibb); Dolfini et al., J. Med. Chem. 14, 117 (1971). Activity studies: Basch et al., Infect. Immun. 4, 44 (1971); Gadebusch et al., ibid. 50. Clinical trials: Woodruff et al., N. Y. State J. Med. 71, 1087 (1971); Beck et al., Curr. Ther. Res. 13, 530 (1971); Reyes, ibid. 602; Landa, ibid. 654.

Cloxacillin CAS Registry Number: 61-72-3 氯唑西林

CAS Name: (2S,5R,6R)-6-[[[3-(2-Chlorophenyl)-5-methyl-4-isoxazolyl]carbonyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Additional Names: [3-(o-chlorophenyl)-5...
Literature References: Semi-synthetic antibiotic related to penicillin; chlorinated deriv of oxacillin, q.v. Prepn: F. P. Doyle, J. H. C. Nayler, US 2996501 (1961); F. P. Doyle et al., J. Chem. Soc. 1963, 5838. Manuf: Ind. Chem. 39, 513 (1963), C.A. 60, 1543a (1964). Properties and pharmacology: J. H. C. Nayler et al., Nature 195, 1264 (1962). Toxicity data: E. I. Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971). Comprehensive description: D. L. Mays, Anal. Profiles Drug Subs. 4, 113-136 (1975).