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

Enfenamic Acid CAS Registry Number: 23049-93-6 2-[(2-苯乙基)氨基]苯甲酸

CAS Name: 2-[(2-Phenylethyl)amino]benzoic acid
Additional Names: N-phenethyl anthranilic acidTrademarks: Tromaril (Unichem)
Percent Composition: C 74.67%, H 6.27%, N 5.80%, O 13.26%
Literature References: Nonsteroidal anti-inflammatory, antipyretic, analgesic. Prepn: S. R. Hashim et al., IN 103066 and IN 114805 (both 1974 to Council Sci. Ind. Res.). Chemistry and pharmacology: P. Sisoda et al., Proc. Symp. CNS Drugs (Council of Scientific and Industrial Research, New Delhi, 1966) pp 238-248. Antithrombotic activity in rheumatoid arthritis and myocardial infarction: S. R. Manikeri et al., Indian J. Med. Res. 71, 438 (1980). Natriuretic activity: N. Kshirsagar et al., Br. J. Clin. Pharmacol. 9, 530 (1980). Clinical trial in nephrotic syndrome: eidem, Indian J. Med. Res. 70, 801 (1979); as postpartum analgesic: S. Tandon et al., Indian Med. Gaz. 116, 182 (1982).

Flunoxaprofen CAS Registry Number: 66934-18-7 氟诺洛芬

CAS Name: (aS)-2-(4-Fluorophenyl)-a-methyl-5-benzoxazoleacetic acidTrademarks: Priaxim (Ravizza)
Percent Composition: C 67.36%, H 4.24%, F 6.66%, N 4.91%, O 16.83%
Literature References: Nonsteroidal anti-inflammatory. Prepn of racemate: D. Evans et al., DE 2324443; eidem, US 3912748 (1973, 1975 both to Lilly). Prepn of racemate and anti-inflammatory activity: D. W. Dunwell et al., J. Med. Chem. 18, 53-58 (1975). Improved process for prepn of racemate and enantiomers: F. Mauri, R. Signorini, BE 877887; eidem, US 4304918 (1979, 1981 both to Ravizza); R. Signorini, A. Verga, DE 3325672 (1984 to Ravizza). HPLC determn of enantiomers in body fluids: S. Pedrazzini et al., J. Chromatogr. 415, 214 (1987). Prophylactic and therapeutic treatment of asthma and other immediate hypersensitivity diseases: W. Dawson, US 4416892 (1983 to Lilly).

Tiaprofenic Acid CAS Registry Number: 33005-95-7 噻洛芬酸

CAS Name: 5-Benzoyl-a-methyl-2-thiopheneacetic acid
Additional Names: a-methyl-5-benzoyl-2-thienylacetic acidTrademarks: Suralgan (Poli); Surgam (HMR)
Percent Composition: C 64.60%, H 4.65%,...
Literature References: Non-steroidal anti-inflammatory. Prepn: F. Clémence, O. Le Martret, DE 2055264 and FR 2112111 (1971 and 1972 to Roussel-UCLAF), C.A. 75, 63597u (1971) and 78, 97473c (1973); F. Clémence et al., Eur. J. Med. Chem. - Chim. Ther. 9, 390 (1974). Pharmacology: eidem, ibid.; H. Fujimura et al., Oyo Yakuri 9, 715 (1975), C.A. 83, 188321w (1975). Review of pharmacology and efficacy in rheumatic diseases and pain control: E. M. Sorkin, R. N. Brogden, Drugs 29, 208-235 (1985).

Ximoprofen CAS Registry Number: 56187-89-4 希莫洛芬

CAS Name: 4-[3-(Hydroxyimino)cyclohexyl]-a-methylbenzeneacetic acid
Additional Names: p-(3-oxocyclohexyl)hydratropic acid oxime; XIFAM; 2-[4-(3-oximinocyclohexyl)phenyl]propionic acidPercent Co...
Literature References: Nonsteroidal anti-inflammatory. Prepn: J. G. Maillard, DE 2442910; idem, US 3935255 (1975, 1976 both to Lab. Jacques Logeais). Metabolism: B. C. Mayo et al., Xenobiotica 20, 233 (1990). Clinical pharmacokinetics: I. W. Taylor et al., Br. J. Clin. Pharmacol. 32, 242 (1991). GC determn in plasma: I. W. Taylor, L. F. Chasseaud, J. Chromatogr. 495, 275 (1989). HPLC determn in urine: G. R. Morris et al., ibid. 530, 377 (1990). Clinical evaluation: M. Dougados et al., J. Rheumatol. 16, 1167 (1989).

Pirprofen CAS Registry Number: 31793-07-4 吡咯布洛芬

CAS Name: 3-Chloro-4-(2,5-dihydro-1H-pyrrol-1-yl)-a-methylbenzeneacetic acid
Additional Names: 3-chloro-4-(3-pyrrolin-1-yl)hydratropic acidTrademarks: Rangasil (Novartis); Rengasil (Novartis); ...
Literature References: Non-steroidal anti-inflammatory. Prepn: R. W. Carney, G. DeStevens, US 3641040 (1972 to Ciba); R. W. Carney et al., Experientia 29, 938 (1973). Metabolism: R. C. Luders et al., Clin. Pharmacol. Ther. 21, 721 (1977). Pharmacology: G. Wilhelmi, Pharmacology 16, 268 (1978). Pharmacokinetics: M. Beth et al., J. Clin. Pharmacol. 15, 563 (1975). Comparative efficacy: R. J. Saykaly et al., ibid. 19, 59 (1979). Review of pharmacology and therapeutic efficacy: P. A. Todd, R. Beresford, Drugs 32, 509-537 (1986).

Tamoxifen CAS Registry Number: 10540-29-1 他莫昔芬

CAS Name: (Z)-2-[4-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethanamine
Additional Names: 1-p-b-dimethylaminoethoxyphenyl-trans-1,2-diphenylbut-1-ene
Percent Composition: C 84.06%, H 7.87...
Literature References: Nonsteroidal estrogen antagonist. Prepn: BE 637389 (1964 to ICI). Identification and separation of isomers: G. R. Bedford, D. N. Richardson, Nature 212, 733 (1966); BE 678807; M. J. K. Harper et al., US 4536516 (1966, 1985 both to ICI). Stereospecific synthesis: R. B. Miller, M. I. Al-Hassan, J. Org. Chem. 50, 2121 (1985). Review of chemistry and pharmacology: B. J. A. Furr, V. C. Jordan, Pharmacol. Ther. 25, 127-205 (1984). Reviews of clinical experience in treatment and prevention of breast cancer: I. A. Jaiyesimi et al., J. Clin. Oncol. 13, 513-529 (1995); C. K. Osborne, N. Engl. J. Med. 339, 1609-1618 (1998).

Bicalutamide CAS Registry Number: 90357-06-5 比卡鲁胺

CAS Name: N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide
Additional Names: 4-cyano-3-trifluoromethyl-N-(3-p-fluorophenylsulfonyl-2-hydroxy-2-me...
Literature References: Non-steroidal peripherally active antiandrogen. Prepn: H. Tucker, EP 100172; idem, US 4636505 (1984, 1987 both to ICI); and structure-activity: H. Tucker et al., J. Med. Chem. 31, 954 (1988). Resolution and activity of enantiomers: H. Tucker, G. J. Chesterson, ibid. 885. Pharmacokinetics: I. D. Cockshott et al., Eur. Urol. 18, Suppl. 3, 10 (1990). Clinical trials in prostate cancer: G. Lunglmayr, Horm. Res. 32, Suppl. 1, 77 (1989); D. W. W. Newling, Eur. Urol. 18 Suppl. 3, 18 (1990). Review of pharmacology: B. J. A. Furr in Hormonal Therapy of Prostatic Diseases: Basic and Clinical Aspects, M. Motta, M. Serio, Eds. (Mediocom Europe, Milan, 1987) 148-161.

Bazedoxifene CAS Registry Number: 198481-32-2 1-[[4-[2-(氮杂环庚烷-1-基)乙氧基]苯基]甲基]-2-(4-羟基苯基)-3-甲基-吲哚-5-醇

CAS Name: 1-[[4-[2-(Hexahydro-1H-azepin-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-o1
Additional Names: 1-[4-(2-azepan-1-ylethoxy)benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H...
Literature References: Nonsteroidal selective estrogen receptor modulator (SERM). Prepn: C. P. Miller et al., EP 802183; eidem, US 5998402 (1997, 1999 both to American Home); C. P. Miller et al., J. Med. Chem. 44, 1654 (2001). Pharmacology and receptor binding study: B. S. Komm et al., Endocrinology 146, 3999 (2005). Clinical pharmacology: S. Ronkin et al., Obstet. Gynecol. 105, 1397 (2005). Review of development: B. S. Komm, C. R. Lyttle, Ann. N.Y. Acad. Sci. 949, 317-326 (2001); and therapeutic potential: C. Gruber, D. Gruber, Curr. Opin. Invest. Drugs 5, 1086-1093 (2004).

Dimestrol CAS Registry Number: 130-79-0 alpha,alpha'-二乙基-4,4'-二甲氧基二苯乙烯

CAS Name: 1,1'-[(1E)-1,2-Diethyl-1,2-ethenediyl]bis[4-methoxybenzene]
Additional Names: (E)-a,a'-diethyl-4,4'-dimethoxystilbene; stilbestrol dimethyl ether; (E)-3,4-bis(p-methoxyphenyl)-3-hexen...
Literature References: Nonsteroidal synthetic estrogen; dimethyl ether of diethylstilbestrol, q.v. Prepn: Dodds et al., Nature 142, 211, 247 (1938); Reid, Wilson, J. Am. Chem. Soc. 64, 1625 (1942); Sisido, Nozaki, J. Am. Chem. Soc. 70, 777 (1948). Improved stereospecific prepn: T. Hiyama, H. Nozaki, Bull. Chem. Soc. Jpn. 46, 2248 (1973). Crystal structure: G. Ruban, P. Luger, Acta Crystallogr. B31, 2658 (1975). Biological activities: Y. Inamori et al., Chem. Pharm. Bull. 33, 4478 (1985). Review and bibliography: Solmssen, Chem. Rev. 37, 481 (1945).

Raloxifene CAS Registry Number: 84449-90-1 雷洛昔芬

CAS Name: [6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]methanone
Additional Names: keoxifenePercent Composition: C 71.01%, H 5.75%, N 2.96%, O 13.51%, S 6...
Literature References: Nonsteroidal, selective estrogen receptor modulator (SERM). Prepn: C. D. Jones, EP 62503; idem, US 4418068 (1982, 1983 both to Lilly); idem et al., J. Med. Chem. 27, 1057 (1984). Review of pharmacology and toxicology: J. Buelke-Sam et al., Reprod. Toxicol. 12, 217-221 (1998); of clinical pharmacology and pharmacokinetics: D. Hochner-Celnikier, Eur. J. Obstet. Gynecol. Reprod. Biol. 85, 23-29 (1999); of clinical efficacy in osteoporosis: D. Agnusdei, ibid. 43-46. Clinical effect on risk of breast cancer: S. R. Cummings et al., J. Am. Med. Assoc. 281, 2189 (1999); on reduction of fracture risk: B. Ettinger et al., ibid. 282, 637 (1999).