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

Tazobactam CAS Registry Number: 89786-04-9 三唑巴坦

CAS Name: (2S,3S,5R)-3-Methyl-7-oxo-3-(1H-1,2,3-triazol-1-ylmethyl)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid 4,4-dioxide
Additional Names: 2b-[(1,2,3-triazol-1-yl)methyl]-2a-methylpe...
Literature References: b-Lactamase inhibitor. Prepn: R. G. Micetich et al., EP 97446; eidem, US 4562073 (1984, 1985 both to Taiho); R. G. Micetich et al., J. Med. Chem. 30, 1469 (1987). Degradation in solution: T. Marunaka et al., Chem. Pharm. Bull. 36, 4478 (1988); in solid state: E. Matsushima et al., ibid. 4593. b-Lactamase inhibiting activity in comparison with clavulanic acid and sulbactam, q.q.v., vs aerobes: M. R. Jacobs et al., Antimicrob. Agents Chemother. 29, 980 (1986); vs anaerobes: P. C. Appelbaum et al., ibid. 30, 789. HPLC determn in biological materials: T. Marunaka et al., J. Chromatogr. 431, 87 (1988). Clinical trial in combination with piperacillin, q.v.: I. M. Gould et al., Drugs Exp. Clin. Res. 17, 187 (1991).

TAED CAS Registry Number: 10543-57-4 四乙酰乙二胺

CAS Name: N,N'-1,2-ethanediylbis[N-acetylacetamide]
Additional Names: N,N,N',N'-tetraacetylethylenediaminePercent Composition: C 52.62%, H 7.07%, N 12.27%, O 28.04%
Literature References: Bleach activator for peroxide-based detergents. Prepn: A. P. N. Franchimont, J. V. Dubsky, Rec. Trav. Chim. 30, 184 (1911); R. P. Mariella, K. H. Brown, J. Org. Chem. 36, 735 (1971). Chemical degradation studies: D. M. Davies, M. E. Deary, J. Chem. Soc. Perkin Trans. 2 1991, 1549; N. Brand et al., Chemosphere 34, 2637 (1997). Determn by iodometric titration in household detergents: L. Baini et al., Riv. Ital. Sostanze Grasse 69, 615 (1992). Biocidal efficacy: V. B. Cloud, I. M. George, Household Pers. Prod. Ind. 34, 82 (1997). Enhancement of whiteness of cellulosic blends: A. J. Mathews, S. J. Scarborough, Proc. Beltwide Cotton Conf. 1998, 732; of wool/cotton blends: P. A. Duffield et al., ibid., 816; of paper pulp: C. Leduc et al., Appita J. 51, 306 (1998).

Bis(pinacolato)diborane CAS Registry Number: 73183-34-3 双戊酰二硼

CAS Name: 4,4,4',4',5,5,5',5'-Octamethyl-2,2'-bi-1,3,2-dioxaborolane
Additional Names: Miyaura's reagent; pinacol diborane; 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-1-yl-4',4',5',5'-tetramethyl-1...
Literature References: Boron source for organic syntheses. Prepn and crystal structure: H. Nöth, Z. Naturforsch. 39b, 1463 (1984). Synthesis: T. Ishiyama et al., Org. Synth. 77, 176 (2000). NMR spectroscopic data: W. Biffar et al., Ber. 113, 333 (1980). First use as boron source in Pt-catalyzed diboration of alkynes: T. Ishiyama et al., J. Am. Chem. Soc. 115, 11018 (1993). Stereospecific synthesis via cross coupling with aromatic amine: C. Malan, C. Morin, J. Org. Chem. 63, 8019 (1998). Rh-catalyzed activation of the C-H bond: Y. Kondo et al., J. Am. Chem. Soc. 124, 1164 (2002). Brief review: X. Liu, Synlett 2003, 2442-2443.

Garner's Aldehyde CAS Registry Number: 127589-93-9 4-甲酰基-2,2-二甲基恶唑烷-3-羧酸叔丁酯

CAS Name: 4-Formyl-2,2-dimethyl-3-oxazolidinecarboxylic acid 1,1-dimethylethyl ester
Additional Names: 1,1-dimethylethyl 4-formyl-2,2-dimethyloxazolidine-3-carboxylate
Percent Composition: C...
Literature References: Both enantiomers are configurationally stable building blocks for use in asymmetric synthesis. Prepn of R-form: P. Garner, Tetrahedron Lett. 25, 5855 (1984); of S-form: P. Garner, J. M. Park, J. Org. Chem. 52, 2361 (1987). Improved prepn of S-form: A. McKillop et al., Synthesis 1994, 31. Review of chemistry: X. Liang et al., J. Chem. Soc. Perkin Trans. 1 2001, 2136-2157.

Rimonabant CAS Registry Number: 168273-06-1 利莫纳班

CAS Name: 5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-carboxamide
Additional Names: N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H...
Literature References: Brain cannabinoid receptor (CB1) antagonist. Prepn: F. Barth et al., EP 576357; eidem., US 5624941 (1993, 1997 both to Sanofi); H. H. Seltzman et al., J. Chem. Soc. Chem. Commun. 1995, 1549; and pharmacology: A. K. Dutta et al., Med. Chem. Res. 5, 54 (1994). Receptor antagonist activity: M. Rinaldi-Carmona et al., FEBS Lett. 350, 240 (1994). Clinical trial in blockade of effects of smoked marijuana: M. A. Huestis et al., Arch. Gen. Psychiatry 58, 322 (2001). Clinical trials in obesity: L. F. Van Gaal et al., Lancet 365, 1389 (2005); J.-P. Després et al., N. Engl. J. Med. 353, 2121 (2005). Review of therapeutic potential in obesity and drug addiction: M. A. M. Carai et al., Life Sci. 77, 2339-2350 (2005).

Rivastigmine CAS Registry Number: 123441-03-2 利凡斯的明

CAS Name: Ethylmethylcarbamic acid 3-[(1S)-1-(dimethylamino)ethyl]phenyl ester
Additional Names: (S)-N-ethyl-3-[(1-dimethylamino)ethyl]-N-methylphenylcarbamate
Percent Composition: C 67.17%,...
Literature References: Brain selective acetylcholinesterase inhibitor. Prepn: A. Enz, DE 3805744; idem, US 5602176 (1988, 1997 both to Sandoz); and activity: R. Amstutz et al., Helv. Chim. Acta 73, 739 (1990). Pharmacology: A. Enz et al., Prog. Brain Res. 98, 431 (1993). Clinical trial in Alzheimer's disease: M. Rösler et al., Br. Med. J. 318, 633 (1999).

Dolasetron CAS Registry Number: 115956-12-2 多拉司琼

CAS Name: 1H-Indole-3-carboxylic acid (2a,6a,8a,9ab)-octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester
Additional Names: endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4...
Literature References: Bridged pseudopelletierine derivative; specific serotonin (5HT3) receptor antagonist. Prepn: M. W. Gittos, EP 266730; idem et al., US 4906755 (1988, 1990 both to Merrell Dow). Binding study: P. H. Boeijinga et al., Eur. J. Pharmacol. 219, 9 (1992). Pharmacology: R. C. Miller et al., Drug Dev. Res. 28, 87 (1993). Clinical pharmacokinetics: H. Boxenbaum et al., Biopharm. Drug Dispos. 13, 693 (1992); eidem, ibid. 14, 131 (1993). GC-MS and LC determn in plasma: T. A. Gillespie et al., J. Pharm. Biomed. Anal. 11, 955 (1993). Clinical trial in emetogenic chemotherapy: A. A. Fauser et al., Eur. J. Cancer 32A, 1523 (1996); for prevention of postoperative nausea: S. G. Graczyk et al., Anesth. Analg. 84, 325 (1997).

Apramycin CAS Registry Number: 37321-09-8 阿布拉霉素

CAS Name: O-4-Amino-4-deoxy-a-D-glucopyranosyl-(1®8)-O-(8R)-2-amino-2,3,7-trideoxy-7-(methylamino)-D-glycero-a-D-allo-octodialdo-1,5:8,4-dipyranosyl-(1®4)-2-deoxy-D-streptamine
Additional Names...
Literature References: Broad spectrum aminocyclitol antibiotic and component of the nebramycin complex, produced by a strain of Streptomyces tenebrarius: R. Q. Thompson, E. A. Presti, Antimicrob. Agents Chemother. 1967, 332; W. M. Stark, US 3691279 (1972 to Lilly). Structure, abs config and properties: S. O'Connor et al., J. Org. Chem. 41, 2087 (1976). 13C-NMR: E. Wenkert, E. W. Hagaman, ibid. 701. In vitro activity: R. Ryden et al., J. Antimicrob. Chemother. 3, 609 (1977). Synthetic studies: H. C. Jarrell, W. A. Szarek, Carbohydr. Res. 67, 43 (1978); eidem, Can. J. Chem. 56, 144 (1978); 57, 924 (1979). See also tobramycin.

Ceftezole CAS Registry Number: 26973-24-0 头孢替唑

CAS Name: (6R,7R)-8-Oxo-7-[(1H-tetrazol-1-ylacetyl)amino]-3-[(1,3,4-thiadiazol-2-ylthio)methyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Additional Names: 7-(1H-tetrazol-1-yl)aceta...
Literature References: Broad spectrum antibiotic similar to cefazolin, q.v. Prepn: T. Takano et al., ZA 6804513; eidem, US 3516997 (1969, 1970 both to Fujisawa). In vitro and in vivo activity: T. Noto et al., J. Antibiot. 29, 1058 (1976). Pharmacology: Y. Harada et al., ibid. 1071; M. Kakimoto et al., Chemotherapy (Tokyo) 24, 722 (1976). Metabolism: K. Koyama et al., ibid. 619; Y. Tohira et al., ibid. 655. Clinical study: S. Ishiyama et al., ibid. 1006. Toxicity and teratogenicity studies: R. Niki et al., ibid. 671.

Polihexanide CAS Registry Number: 32289-58-0; 28757-47-3 (base) 聚六亚甲基双胍盐酸盐

CAS Name: Poly(iminocarbonimidoyliminocarbonimidoylimino-1,6-hexanediyl) hydrochloride
Additional Names: polyaminopropylbiguanide; polyhexamethylene biguanide hydrochloride; polyhexanide; PHMB<...
Literature References: Broad spectrum antimicrobial polymer; binds and disrupts cytoplasmic membranes. Prepn: F. L. Rose, G. Swain, US 2643232 (1953 to ICI). Antibacterial action: A. Davies et al., J. Appl. Bacteriol. 31, 448 (1968). Synthesis and characterization of solution behavior: G. C. East et al., Polymer 38, 3973 (1997). Interactions with phospholipid membranes: P. Broxton et al., J. Appl. Bacteriol. 57, 115 (1984); T. Ikeda et al., Bull. Chem. Soc. Jpn. 58, 705 (1985). Mechanism of action study: W. Khunkitti et al., J. Appl. Microbiol. 82, 107 (1997). Titrimetric determn of biguanide groups: T. Hattori et al., Anal. Sci. 19, 1525 (2003). Clinical evaluation of mouthrinse formulations on bacterial count and plaque growth: M. Rosin et al., J. Clin. Periodontol. 28, 1121 (2001); 29, 392 (2002).