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

Cefoxitin CAS Registry Number: 35607-66-0 头孢西丁

CAS Name: (6R,7S)-3-[[(Aminocarbonyl)oxy]methyl]-7-methoxy-8-oxo-7-[(2-thienylacetyl)amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Additional Names: 3-(hydroxymethyl)-7-methoxy-8...
Literature References: Semi-synthetic antibiotic derived from cephamycin C, q.v., possessing high resistance to b-lactamase inactivation. Synthesis: B. G. Christensen et al., DE 2129675; DE 2203653; eidem, US 4297488 (1971, 1972, 1981 all to Merck Co.); Karady et al., J. Am. Chem. Soc. 94, 1410 (1972); Ratcliffe, Christensen, Tetrahedron Lett. 1973, 4653. Biological evaluation: Wallick, Hendlin, Antimicrob. Agents Chemother. 5, 25 (1974); Miller et al., ibid. 33; Onishi et al., ibid. 38; Hamilton, Miller et al., J. Antibiot. 27, 42 (1974). Mode of action: Onishi et al., Ann. N.Y. Acad. Sci. 235, 406 (1974). Toxicity: S. Takayama et al., Chemotherapy (Tokyo) 26, Suppl. 1, 150 (1978). Comprehensive reviews: J. Antimicrob. Chemother. 4, Suppl. B, 1-256 (1978); R. N. Brogden et al., Drugs 17, 1-37 (1979); E. O. Stapley, K. R. Brown, in Pharmacological and Biochemical Properties of Drug Substances vol. 3, M. E. Goldberg, Ed. (Am. Pharm. Assoc., Washington, DC, 1981) pp 262-290. Comprehensive description: G. S. Brenner, Anal. Profiles Drug Subs. 11, 169-195 (1982). Symposium on therapeutic use in anaerobic and aerobic infectons: Hosp. Pract. 25, Suppl. 4, 1-56 (1990).

Rifamycin SV CAS Registry Number: 6998-60-3 利福霉素

CAS Name: 5,6,9,17,19,21-Hexahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-2,7-(epoxypentadeca[1,11,13]trienimino)naphtho[2,1-b]furan-1,11(2H)-dione 21-acetate
Additional Names: rifomycin S...
Literature References: Semi-synthetic antibiotic derived from Rifamycin S. Prepn: Sensi et al., Experientia 16, 412 (1960); Farmaco Ed. Sci. 16, 165 (1961). Comprehensive review: Bergamini, Fowst, Arzneim.-Forsch. 15, 951-1002 (1965). For general refs see Rifamycins.

Dihydrostreptomycin CAS Registry Number: 128-46-1 双氢链霉素

CAS Name: O-2-Deoxy-2-(methylamino)-a-L-glucopyranosyl-(1®2)-O-5-deoxy-3-C-(hydroxymethyl)-a-L-lyxofuranosyl-(1®4)-N,N'-bis(aminoiminomethyl)-D-streptamine
Additional Names: DHSM; DST
Tradem...
Literature References: Semi-synthetic antibiotic prepd by reduction of streptomycin: Bartz et al., J. Am. Chem. Soc. 68, 2163 (1946); Fried, Wintersteiner, ibid. 69, 79 (1947); Peck, US 2498574 (1950 to Merck Co.); Carboni, Regna, US 2522858 (1950 to Pfizer); Levy, US 2663685 (1953 to Schenley); Dolliver, Semenoff, US 2717236 (1955 to Olin Mathieson); Kaplan, US 2790792 (1957 to Bristol); Sokol, Popino, US 2784181 (1957 to Cyanamid); Jurist, US 2945850 (1960 to Olin Mathieson). Isoln from fermentation broth of Streptomyces humidus: Nakazawa et al., and Tatsuoka et al., US 2931756 and US 2950277 (both 1960 to Takeda). Crystn of free base (obtained from the sulfate): Rhodehamel et al., Science 111, 233 (1950). Crystn of the hydrochloride: Wolf et al., ibid. 109, 515 (1949); Wolf, US 2590139; US 2594245 (both 1952 to Merck Co.). Crystn of the sulfate: Solomons, Regna, Science 109, 515 (1949); Wolf et al., ibid. 515; Wolf, US 2590140; US 2590141 (both 1952 to Merck Co.); R. B. Peet, US 2640054 (1953 to Heyden Chem.); Katz, US 2744892 (1956 to Schenley). Total synthesis: Umezawa et al., J. Am. Chem. Soc. 96, 920 (1974); eidem, Bull. Chem. Soc. Jpn. 48, 563 (1975); T. Yamasaki et al., J. Antibiot. 31, 1233 (1978).

Streptonicozid CAS Registry Number: 5667-71-0

CAS Name: 4-Pyridinecarboxylic acid hydrazide, hydrazone with O-2-deoxy-2-(methylamino)-a-L-glucopyranosyl-(1®2)-O-5-deoxy-3-C-formyl-a-L-lyxofuranosyl-(1®4)-N,N'-bis(aminoiminomethyl)-D-streptami...
Literature References: Semi-synthetic antibiotic prepd by the condensation of streptomycin salts and isonicotinic acid hydrazide in methanol: Pennington et al., J. Am. Chem. Soc. 75, 2261 (1953).

Clindamycin CAS Registry Number: 18323-44-9 克林霉素

CAS Name: Methyl 7-chloro-6,7,8-trideoxy-6-[[[(2S,4R)-1-methyl-4-propyl-2-pyrrolidinyl]carbonyl]amino]-1-thio-L-threo-a-D-galacto-octopyranoside
Additional Names: 7(S)-chloro-7-deoxylincomycin;...
Literature References: Semi-synthetic antibiotic prepd from lincomycin, q.v. Prepn: Magerlein et al., Antimicrob. Agents Chemother. 1966, 727. Manuf process: R. D. Birkenmeyer, US 3475407 (1969 to Upjohn). Synthesis and structure: R. D. Birkenmeyer, F. Kagan, J. Med. Chem. 13, 616 (1970). Stability studies: Oesterling, J. Pharm. Sci. 59, 63 (1970). Activity studies: McGehee et al., Am. J. Med. Sci. 256, 279 (1968); D. A. Leigh, J. Antimicrob. Chemother. 7(suppl. A), 3 (1981). Toxicology: J. E. Gray et al., Toxicol. Appl. Pharmacol. 21, 516 (1972). Comprehensive description of the hydrochloride: L. W. Brown, W. F. Beyer, Anal. Profiles Drug Subs. 10, 75-91 (1981).

Rolitetracycline CAS Registry Number: 751-97-3 罗利环素

CAS Name: [4S-(4a,4aa,5aa,6b,12aa)]-4-(Dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-N-(1-pyrrolidinylmethyl)-2-naphthacenecarboxamide
Additional ...
Literature References: Semi-synthetic antibiotic prepd from tetracycline: Siedel et al., Muench. Med. Wochenschr. 100, 661 (1958); Lindner et al., ZA 5703169. Alternate procedure and structure: Gottstein et al., J. Am. Chem. Soc. 81, 1198 (1959); Cheney et al., US 3104240 (1963 to Bristol-Myers). Toxicity: E. I. Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971).

Azidamfenicol CAS Registry Number: 13838-08-9 叠氮氯霉素

CAS Name: 2-Azido-N-[2-hydroxy-1-(hydroxymethyl)-2-(4-nitrophenyl)ethyl]acetamide
Additional Names: D-(-)-threo-1-p-nitrophenyl-2-azidoacetylaminopropane-1,3-diol; D-(-)-threo-2-azidoacetamido-...
Literature References: Semi-synthetic antibiotic related to chloramphenicol, q.v. Prepn: Meiser, Domagk, US 2882275 (1959 to Bayer).

Zorubicin CAS Registry Number: 54083-22-6 佐柔比星

CAS Name: (2S-cis)-Benzoic acid [1-[4-[(3-amino-2,3,6-trideoxy-a-L-lyxo-hexopyranosyl)oxy]-1,2,3,4,6,11-hexahydro-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-2-napthacenyl]ethylidene]hydrazide
Addit...
Literature References: Semi-synthetic antibiotic related to daunorubicin, q.v. Prepn: G. Jolles, DE 2327211 (1974 to Rhone-Poulenc), C.A. 82, 171381x (1975). Biological activity: R. Maral et al., C.R. Seances Acad. Sci. Ser. D 275, 301 (1972); R. Maral, Cancer Chemother. Pharmacol. 2, 31 (1979). Distribution and metabolism in mice: R. Baurain et al., ibid. 37. Mechanism of action: G. P. Sartiano et al., J. Antibiot. 32, 1038 (1979). Acute cardiovascular effects in dogs: E. H. Herman, R. S. Young, Cancer Treat. Rep. 63, 1771 (1979). Clinical study in breast cancer: J. N. Ingle, ibid. 1701.

Amdinocillin Pivoxil CAS Registry Number: 32886-97-8 匹美西林

CAS Name: (2S,5R,6R)-6-[[(Hexahydro-1H-azepin-1-yl)methylene]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 Nam...
Literature References: Semi-synthetic antibiotic related to penicillin. Pivaloyloxymethyl ester of amdinocillin, q.v. Prepn: F. J. Lund, DE 2055531; idem, US 3957764 (1971, 1976 both to Lövens Kemiske Fabrik). HPLC stability analysis: R. B. Hagel, E. H. Waysek, J. Chromatogr. 178, 97 (1979). Bacteriological and pharmacokinetic study: T. Damsgaard et al., J. Antimicrob. Chemother. 5, 267 (1979). Metabolism: J. D. Anderson, M. A. Adams, Chemotherapy 25, 1 (1979). Clinical study: B. T. Andersen et al., Infection 8, 27 (1980). Toxicity study: S. Sato et al., Takeda Kenkyushoho 35, 179 (1976), C.A. 86, 115154w (1977).

Quinacillin CAS Registry Number: 1596-63-0 喹那西林

CAS Name: (2S,5R,6R)-6-[[(3-Carboxy-2-quinoxalinyl)carbonyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Additional Names: 3-carboxy-2-quinoxalinylpenicillin Literature References: Semi-synthetic antibiotic related to penicillin. Prepd by condensation of quinoxaline-2,3-dicarboxylic anhydride with 6-aminopenicillanic acid: Richards et al., Nature 199, 354 (1963).