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

Taurolidine CAS Registry Number: 19388-87-5 牛磺罗定

CAS Name: 4,4'-Methylenebis(tetrahydro-1,2,4-thiadiazine) 1,1,1',1'-tetraoxide
Additional Names: 4,4'-methylenebis(perhydro-1,2,4-thiadiazine 1,1-dioxide); bis(1,1-dioxoperhydro-1,2,4-thiadiazi...
Literature References: Broad spectrum, synthetic formaldehyde carrier formed by the condensation of two molecules of taurine and three molecules of formaldehyde. Prepn: FR 1458701; R. W. Pfirrmann, US 3423408 (1966, 1969 both to Ed. Geistlich Söhne). Antibacterial activity in mice: M. K. Browne et al., J. Appl. Bacteriol. 41, 363 (1976). Anti-endotoxin activity in lab animals: R. W. Pfirrmann, G. B. Leslie, ibid. 46, 97 (1979). Mechanism of action: E. Myers et al., ibid. 48, 89 (1980). HPLC determn of metabolites in plasma: A. D. Woolfson et al., Int. J. Pharm. 49, 135 (1989). Pharmacokinetics: C. Steinbach-Lebbin et al., Arzneim.-Forsch. 32, 1542 (1982). Metabolism in humans: B. I. Knight et al., Br. J. Clin. Pharmacol. 12, 695 (1981). Clinical trials in peritonitis: M. K. Browne et al., Surg. Gynecol. Obstet. 146, 721 (1978); G. Wesch et al., Fortschr. Med. 101, 545 (1983); in wound sepsis: A. K. Halsall et al., Pharmatherapeutica 2, 673 (1981); in pleural infection: A. A. Conlan et al., S. Afr. Med. J. 64, 653 (1983).

Cefditoren CAS Registry Number: 104145-95-1 头孢妥仑酸

CAS Name: (6R,7R)-7-[[(2Z)-(2-Amino-4-thiazolyl)(methoxyimino)acetyl]amino]-3-[(1Z)-2-(4-methyl-5-thiazolyl)ethenyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Additional Names...
Literature References: Broad spectrum, third generation cephalosporin; active metabolite of orally absorbed pivaloyloxymethyl ester prodrug. Prepn: K. Atsumi et al., EP 175610; eidem, US 4839350 (1986, 1989 both to Meiji); K. Sakagami et al., J. Antibiot. 43, 1047 (1990); idem et al., Chem. Pharm. Bull. 39, 2433 (1991). In vitro and in vivo activities: A. Tamura et al., Antimicrob. Agents Chemother. 32, 1421 (1988). Extensive in vitro activity study: D. Felmingham et al., Drugs Exp. Clin. Res. 20, 127 (1994). Clinical pharmacokinetics and efficacy in pediatrics: N. Iwai et al., Jpn. J. Antibiot. 47, 181 (1994), C.A. 120, 260636e (1994).

Cefotetan CAS Registry Number: 69712-56-7 头孢替坦

CAS Name: (6R,7S)-7-[[[4-(2-Amino-1-carboxy-2-oxoethylidene)-1,3-dithietan-2-yl]carbonyl]amino]-7-methoxy-3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-ca...
Literature References: Broad-spectrum injectable semi-synthetic antibiotic derived from cephamycin C, q.v. Prepn: M. Iwanami et al., DE 2824559; eidem, US 4263432 (1979, 1981 both to Yamanouchi); eidem, Chem. Pharm. Bull. 28, 2629 (1980). Commercial-scale synthesis: M. Fujimoto et al., Org. Process Res. Dev. 8, 915 (2004). In vitro comparison of antibacterial activity: B. Chattopadhyay, J. C. Teli, J. Antimicrob. Chemother. 10, 151 (1982). Toxicity study: K. Imamura et al., Chemotherapy (Tokyo) 30, Suppl. 1, 212 (1982). Series of articles on pharmacology, clinical studies, toxicology: ibid. 1-947; J. Antimicrob. Chemother. 11, Suppl. A, 1-236 (1983). Review of antibacterial activity, pharmacokinetics, therapeutic use: A. Ward, D. M. Richards, Drugs 30, 382-426 (1985).

Cefamandole CAS Registry Number: 34444-01-4 头孢孟多

CAS Name: (6R,7R)-7-[[(2R)-Hydroxyphenylacetyl]amino]-3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Additional Names: 7-mandelamido-3-[...
Literature References: Broad-spectrum semi-synthetic cephalosporin antibiotic. Prepn: C. W. Ryan, DE 2018600; idem, US 3641021 (1970, 1972 to Lilly); J. M. Greene, DE 2312997; idem, US 3840531 (1973, 1974 to Lilly). Biological properties: W. E. Wick, D. A. Preston, Antimicrob. Agents Chemother. 1, 221 (1972). Antibacterial activity: S. Eykyn et al., ibid. 3, 657 (1973); H. C. Neu, ibid. 6, 177 (1974); A. D. Russell, J. Antimicrob. Chemother. 1, 97 (1975). Pharmacologic studies: B. R. Meyers et al., Antimicrob. Agents Chemother. 9, 140 (1976); R. S. Griffith et al., ibid. 10, 814 (1976). Comprehensive description: R. H. Bishara, E. C. Rickard, Anal. Profiles Drug Subs. 9, 125-154 (1980).

Prodiamine CAS Registry Number: 29091-21-2 氨氟乐灵

CAS Name: 2,4-Dinitro-N3,N3-dipropyl-6-(trifluoromethyl)-1,3-benzenediamine
Additional Names: a,a,a-trifluoro-3,5-dinitro-N4,N4-dipropyltoluene-2,4-diamine; 5-dipropylamino-a,a,a-trifluoro-4,6-...
Literature References: Broad-spectrum, pre-emergence dinitroaniline herbicide. Prepn: D. L. Hunter et al., DE 2013510; eidem, US 3764623 (1970, 1973 both to U.S. Borax and Chemical Corp.). Weed control in container grown plants: T. A. Fretz, W. J. Sheppard, HortScience 15, 489 (1980); S. A. Duray, F. T. Davies, J. Environ. Hort. 5, 82 (1987). Field studies: M. G. Sybouts, Proc. West. Soc. Weed Sci. 40, 169 (1987). Evaluation of herbicidal activity: W. Bond, Crop Prot. 7, 75 (1988). Review of herbicidal activity: S. J. Bowe, Proc. West. Soc. Weed Sci. 39, 216-218 (1986).

Bromperidol CAS Registry Number: 10457-90-6 溴哌利多

CAS Name: 4-[4-(4-Bromophenyl)-4-hydroxy-1-piperidinyl]-1-(4-fluorophenyl)-1-butanone
Additional Names: 4-[4-(p-bromophenyl)-4-hydroxypiperidino]-4'-fluorobutyrophenoneTrademarks: Azurene (Cila...
Literature References: Bromine analog of haloperidol, q.v. Prepn (no data): P. A. J. Janssen, GB 895309; idem, US 3438991 (1962, 1969 both to Janssen); C. J. E. Niemegeers, P. A. J. Janssen, Arzneim.-Forsch. 24, 45 (1974). Prepn of 82Br bromperidol and preliminary tissue distribution studies: S. H. Vincent et al., J. Med. Chem. 23, 75 (1980). Pharmacological study: C. J. E. Niemegeers, P. A. J. Janssen, Life Sci. 24, 2201 (1979). Preliminary clinical study: B. Woggon et al., Int. Pharmacopsychiatry 14, 213 (1979). Radioimmunoassay: E. Van Den Eeckhout et al., Eur. J. Drug Metab. Pharmacokinet. 5, 45 (1980).

Timiperone CAS Registry Number: 57648-21-2 替米哌隆

CAS Name: 4-[4-(2,3-Dihydro-2-thioxo-1H-benzimidazol-1-yl)-1-piperidinyl]-1-(4-fluorophenyl)-1-butanone
Additional Names: 1-[1-[3-(4-fluorobenzoyl)propyl]-4-piperidyl]-2-mercaptobenzimidazole; ...
Literature References: Butyrophenone derivative with neuroleptic activity. Prepn: M. Sato et al., JP Kokai 75 84578; K. Ueno et al., US 3963727 (1975, 1976 both to Daiichi); M. Sato et al., J. Med. Chem. 21, 1116 (1978). Improved synthesis: M. Sato, M. Arimoto, Chem. Pharm. Bull. 30, 719 (1982). Pharmacology: T. Yamasaki et al., Jpn. J. Pharmacol. 27 (Suppl.), 124P (1977); eidem, Arzneim.-Forsch. 31, 701, 707 (1981); T. Shibuya et al., Int. J. Clin. Pharmacol. Ther. Toxicol. 20, 251 (1982). Pharmacokinetics and metabolism: H. Tachizawa et al., Drug Metab. Dispos. 9, 442 (1981); K. Sudo et al., Xenobiotica 11, 685 (1981). Multicenter controlled clinical trials in schizophrenia: R. Takahashi et al., J. Int. Med. Res. 10, 257 (1982); T. Kariya et al., ibid. 11, 66 (1983).

Strophanthidin CAS Registry Number: 66-28-4 毒毛旋花子苷元

CAS Name: (3b,5b)-3,5,14-Trihydroxy-19-oxocard-20(22)-enolide
Additional Names: apocynamarin; convallatoxigenin; corchorin; cymarigenin; cynotoxin; corchorgenin; corchsularin
Percent Composi...
Literature References: By acid or enzymic hydrolysis of glycosides present in several species of Strophanthus, Apocynaceae. Isoln: Jacobs, Heidelberger, J. Biol. Chem. 54, 253 (1922). Structure: Kon, Chem. Ind. (London) 53, 593, 956 (1934); Jacobs, Elderfield, Science 80, 533 (1934). Identity with corchorin, corchorgenin and corchsularin: Sen et al., Helv. Chim. Acta 40, 588 (1957). Synthesis from pregnenolone acetate, q.v.: E. Yoshii et al., J. Org. Chem. 43, 3946 (1978). Toxicity study: Graebner, Geisel, Arzneim.-Forsch. 22, 1854 (1972). Reviews: Elderfield, Chem. Rev. 17, 187 (1935); Tschesche, Ergeb. Physiol. 38, 31 (1936); Stoll, The Cardiac Glycosides (Pharmaceutical Press, London, 1937); Strain in Organic Chemistry vol. II, Gilman, Ed. (New York, 2nd ed., 1943); Fieser, Fieser, Steroids (Reinhold, New York, 1959) pp 729-730, 736-750.

Primeverose CAS Registry Number: 26531-85-1 6-O-beta-D-吡喃木糖基-D-葡萄糖

CAS Name: 6-O-b-D-Xylopyranosyl-D-glucose
Additional Names: 6-(b-D-xylosido)-D-glucose
Percent Composition: C 42.31%, H 6.46%, O 51.24%
Literature References: By enzymatic hydrolysis of gaultherin (monotropitoside), primeverin, rhamnicoside and other glycosides: Goris, Vischniac, Compt. Rend. 169, 871 (1919); Bridel, ibid. 179, 991 (1924); Bridel, Charaux, ibid. 180, 857 (1925); Richter, J. Chem. Soc. 1936, 1701. Synthesis: Helferich, Rauch, Ber. 59, 2655 (1926); Ann. 455, 168 (1927); McCloskey, Coleman, J. Am. Chem. Soc. 65, 1778 (1943).

Vicianose CAS Registry Number: 14116-69-9

CAS Name: 6-O-a-L-Arabinopyranosyl-D-glucose
Additional Names: 6-(a-L-arabinosido)-D-glucose
Percent Composition: C 42.31%, H 6.46%, O 51.24%
Literature References: By enzymatic hydrolysis of vicianin, gein, and violutin: Bertrand, Weisweiller, Compt. Rend. 150, 181 (1910); Bull. Soc. Chim. [4] 9, 38 (1911). Synthesis: Helferich, Bredereck, Ann. 465, 166 (1928); Wallenfels, Beck, Ann. 630, 46 (1960).