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

Flutazolam CAS Registry Number: 27060-91-9 氟恶唑兰

CAS Name: 10-Chloro-11b-(2-fluorophenyl)-2,3,7,11b-tetrahydro-7-(2-hydroxyethyl)oxazolo[3,2-d][1,4]benzodiazepin-6(5H)-oneTrademarks: Coreminal (Mitsui)
Percent Composition: C 60.56%, H 4.81%, ...
Literature References: Tricyclic benzodiazepine deriv. Prepn: BE 765253; M. E. Derieg et al., US 3905956 (1971, 1975 both to Hoffmann-La Roche). Physicochemical properties: A. Ito et al., Iyakuhin Kenkyu 9, 787 (1978), C.A. 89, 169013e (1979). Psychopharmacological profile: T. Mitsushima, S. Ueki, Folia Pharmacol. Jpn. 74, 959 (1978), C.A. 90, 180083u (1979). Toxicological studies: K. Ishimura et al., Oyo Yakuri 15, 1081 (1978); eidem, ibid. 16, 693 (1978), C.A. 90, 16379z, 145909p (1979).

Monatepil CAS Registry Number: 103377-41-9 1-哌嗪丁酰胺,N-(6,11-二氢二苯并[b,e]噻庚英-11-基)-4-(4-氟苯基)-

CAS Name: N-(6,11-Dihydrodibenzo[b,e]thiepin-11-yl)-4-(4-fluorophenyl)-1-piperazinebutanamide
Additional Names: 11-[4-[4-(4-fluorophenyl)-1-piperazinyl]butyrylamino]-6,11-dihydrodibenzo[b,e]thi...
Literature References: Tricyclic calcium channel blocker with a1-adrenoceptor antagonist activity. Prepn: H. Uno et al., WO 8601203; eidem, US 4749703 (1986, 1988 both to Dainippon); M. Kurokawa et al., J. Med. Chem. 34, 927 (1991). HPLC determn in plasma: M. Kurono et al., J. Chromatogr. 532, 175 (1990). Review of pharmacology: H. Takeuchi et al., Cardiovasc. Drug Rev. 12, 254-269 (1994). Series of articles on pharmacology and clinical effect in hypertension and hyperlipidemia: Am. J. Hypertens. 7 (No. 10, pt. 2), 131S-166S (1994).

Tianeptine CAS Registry Number: 66981-73-5 噻奈普汀

CAS Name: 7-[(3-Chloro-6,11-dihydro-6-methyldibenzo[c,f][1,2]thiazepin-11-yl)amino]heptanoic acid S,S-dioxide
Percent Composition: C 57.72%, H 5.77%, Cl 8.11%, N 6.41%, O 14.65%, S 7.34%
Literature References: Tricyclic compound with psychostimulant, anti-ulcer and anti-emetic properties. Prepn: C. Malen et al., DE 2011806 corresp to US 3758528 (1970, 1973 both to Sci. Union et Cie-Soc. Franc. Rech. Med.). Neuropharmacology study: C. Malen, J. Poignant, Experientia 28, 811 (1972).

Lonafarnib CAS Registry Number: 193275-84-2 氯那法尼

CAS Name: 4-[2-[4-[(11R)-3,10-Dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl]-1-piperidinyl]-2-oxoethyl]-1-piperidinecarboxamideTrademarks: Sarasar (Schering-Plough)
...
Literature References: Tricyclic farnesyl protein transferase inhibitor. Prepn: R. J. Doll et al., WO 9723478; eidem, US 5874442 (1997, 1999 both to Schering-Plough); F. G. Njoroge et al., J. Med. Chem. 41, 4890 (1998). Improved prepn: S.-C. Kuo et al., J. Org. Chem. 68, 4984 (2003). Crystal structure of complex with farnesyl protein transferase: C. L. Strickland et al., J. Med. Chem. 42, 2125 (1999). LC/MS/MS determn in plasma: N. M. G. Appels et al., Rapid Commun. Mass Spectrom. 19, 2187 (2005). Antitumor activity in human xenograft and transgenic mouse cancer models: M. Liu et al., Cancer Res. 58, 4947 (1998). Clinical evaluation in cancer: A. A. Adjei et al., ibid. 60, 1871 (2000). Inhibition of P-glycoprotein mediated drug efflux: E. Wang et al., ibid. 61, 7525 (2001). Clinical evaluation with paclitaxel in non-small cell lung cancer: E. S. Kim et al., Cancer 104, 561 (2005).

Ibafloxacin CAS Registry Number: 91618-36-9 依巴沙星

CAS Name: 9-Fluoro-6,7-dihydro-5,8-dimethyl-1-oxo-1H,5H-benzo[ij]quinolizine-2-carboxylic acidPercent Composition: C 65.45%, H 5.13%, F 6.90%, N 5.09%, O 17.44%
Literature References: Tricyclic fluorinated quinolone-type antibacterial; related to flumequine, q.v. Prepn: R. M. Stern, EP 109284; idem, US 4472405 (both 1984 to Riker Labs.). Antimicrobial spectrum: L. J. V. Piddock et al., Eur. J. Clin. Microbiol. 5, 303 (1986); K. V. I. Rolston et al., Eur. J. Clin. Microbiol. Infect. Dis. 7, 681 (1988). Synthesis, absolute configuration and antibacterial activity of enantiomers: J. F. Gerster et al., J. Med. Chem. 30, 839 (1987).

Pirenzepine CAS Registry Number: 28797-61-7 哌仑西平

CAS Name: 5,11-Dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-onePercent Composition: C 64.94%, H 6.02%, N 19.93%, O 9.11%
Literature References: Tricyclic gastric-acid inhibitor. Prepn: FR 1505795 (1967 to Thomae), C.A. 70, 4154w (1969). Pharmacology: W. Eberlein et al., Arzneim.-Forsch. 27, 356 (1977). Pharmacokinetics: R. Hammes et al., ibid. 928. Mechanism of action: G. Heller et al., Verh. Dtsch. Ges. Inn. Med. 84, 991 (1978), C.A. 90, 132984s (1979). Human pharmacology: H. Brunner et al., Arzneim.-Forsch. 27, 684 (1977). Multicenter controlled clinical trial: Scand. J. Gastroenterol. 17, Suppl. 81, 1-42 (1982). Radioimmunoassay determn in human plasma and urine: C. A. Homon et al., Ther. Drug Monit. 9, 236 (1987). Symposium: ibid. Suppl. 72, 1-273. Review of pharmacology and therapeutic efficacy: A. A. Carmine, R. N. Brogden, Drugs 30, 85-126 (1985). Comprehensive description: H. A. El-Obeid et al., Anal. Profiles Drug Subs. 16, 445-506 (1987).

Rapamycin CAS Registry Number: 53123-88-9 雷帕霉素

Additional Names: Sirolimus; RAPA; RPMTrademarks: Rapamune (Wyeth)
Percent Composition: C 67.01%, H 8.71%, N 1.53%, O 22.75%
Literature References: Triene macrolide antibiotic isolated from Streptomyces hygroscopicus. Name derived from the native word for Easter Island, Rapa Nui. Isoln: S. N. Sehgal et al., DE 2347682; eidem, US 3929992 (1974, 1975 both to Ayerst McKenna Harrison); purification and characterization: C. Vézina et al., J. Antibiot. 28, 721 (1975); S. N. Sehgal et al., ibid. 727. Inhibition of immune response: R. R. Martel et al., Can. J. Physiol. Pharmacol. 55, 48 (1977); of graft rejection in mice: C. P. Eng et al., Transplant. Proc. 23, 868 (1991). Total synthesis: K. C. Nicolaou et al., J. Am. Chem. Soc. 115, 4419 (1993); D. Romo et al., ibid. 7906. Series of articles on therapeutic monitoring and pharmacokinetics: Clin. Ther. 22, Suppl. 2, B1-B132 (2000); on pharmacology and clinical experience in transplantation: Transplant. Proc. 35, Suppl. 1, S1-S233 (2003). Clinical trial in prevention of coronary restenosis: D. R. Holmes, Jr. et al., Circulation 109, 634 (2004).

Tosufloxacin CAS Registry Number: 100490-36-6 托弗沙星

CAS Name: 7-(3-Amino-1-pyrrolidinyl)-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acidPercent Composition: C 56.44%, H 3.74%, F 14.10%, N 13.86%, O 11.87%
Literature References: Trifluorinated quinolone antibacterial. Prepn: H. Narita et al., DE 3514076 (1985 to Toyama), C.A. 104, 129888r (1986); D. T. W. Chu, EP 153580; idem, US 4616019 (1985, 1986 both to Abbott); and activity: idem et al., J. Med. Chem. 29, 2363 (1986); H. Narita et al., Yakugaku Zasshi 106, 802 (1986), C.A. 106, 196291v (1987). In vitro activity studies of the base: P. B. Fernandes et al., Antimicrob. Agents Chemother. 32, 27 (1988); and in vivo animal studies of the toluenesulfonate: M. Takahata et al., J. Antimicrob. Chemother. 22, 143 (1988). Series of articles on antibacterial activity and clinical evaluation: Chemotherapy (Tokyo) 36, Suppl. 9, 1-1538 (1988).

Halobetasol Propionate CAS Registry Number: 66852-54-8 卤倍他索丙酸酯

CAS Name: (6a,11b,16b)-21-Chloro-6,9-difluoro-11-hydroxy-16-methyl-17-(1-oxopropoxy)pregna-1,4-diene-3,20-dione
Additional Names: 21-chloro-6a,9-difluoro-11b,17-dihydroxy-16b-methylpregna-1,4-d...
Literature References: Trihalogenated corticosteroid structurally related to clobetasol, q.v. Prepn: J. Kalvoda, G. Anner, DE 2743069; eidem, US 4619921 (1978, 1986 both to Ciba-Geigy). Clinical pharmacology in psoriatic patients: W. A. Watson et al., Pharmacotherapy 10, 107 (1990). Clinical trial in localized vitiligo: L. Xunquan et al., Int. J. Dermatol. 29, 295 (1990).

Mesotrione CAS Registry Number: 104206-82-8 甲基磺草酮

CAS Name: 2-[4-(Methylsulfonyl)-2-nitrobenzoyl]-1,3-cyclohexanedioneTrademarks: Callisto (Syngenta)
Percent Composition: C 49.55%, H 3.86%, N 4.13%, O 33.01%, S 9.45%
Literature References: Triketone herbicide for use in maize; inhibits p-hydroxyphenylpyruvate dioxygenase (HPPD). Synthetic mimic of leptospermone, a natural herbicide produced by the bottlebrush plant, Callistemon citrinus Stapf. Prepn: C. G. Carter, EP 186118 (1986 to Stauffer); idem, US 5006158 (1991 to ICI). Comprehensive description: R. A. Wichert et al., Brighton Crop Prot. Conf. - Weeds 1999, 105-110. HPLC determn in crops, soil, water: P. Alferness, L. Wiebe, J. Agric. Food Chem. 50, 3926 (2002). Adsorption and degradation in soil: J. S. Dyson et al., J. Environ. Qual. 31, 613 (2002). Review: G. Mitchell et al., Pest Manage. Sci. 57, 120-128 (2001).