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

Cyclophosphamide CAS Registry Number: 6055-19-2; 50-18-0 (anhydrous) 环磷酰胺,一水

CAS Name: N,N-Bis(2-chloroethyl)tetrahydro-2H-1,3,2-oxazaphosphorin-2-amine 2-oxide monohydrate
Additional Names: 1-bis(2-chloroethyl)amino-1-oxo-2-aza-5-oxaphosphoridin monohydrate; bis(2-chlo...
Literature References: Oxazaphosphine cytostatic agent; supresses B-cell activity and antibody formation. Prepn: H. Arnold, F. Bourseaux, Angew. Chem. 70, 539 (1958). Optical resolution study: T. Kawashima et al., J. Org. Chem. 43, 1111 (1978). Toxicology: A. G. Wheeler et al., Toxicol. Appl. Pharmacol. 4, 324 (1962). Book: D. L. Hill, A Review of Cyclophosphamide (Charles C Thomas, Springfield, 1975) 340 pp. Reviews of carcinogenicity studies: IARC Monographs 9, 135-156 (1975); of field trials as defleecing agent for sheep: M. H. Fahmy, Y. Moride, Anim. Breed. Abstr. 52, 7-19 (1984); of clinical toxicology: L. H. Fraiser et al., Drugs 42, 781-795 (1991); of mechanism of action and clinical use: O. M. Colvin, Curr. Pharmaceut. Design 5, 555-560 (1999); of analytical methods: M. Malet-Martino et al., ibid. 561-586; and metabolism: F. Baumann, R. Preiss, J. Chromatogr. B 764, 173-192 (2001).

Zoapatanol CAS Registry Number: 71117-51-6

CAS Name: 9-[(2S,3R,6E)-3-Hydroxy-6-(2-hydroxyethylidene)-2-methyl-2-oxepanyl]-2,6-dimethyl-2-nonen-5-one
Percent Composition: C 70.97%, H 10.12%, O 18.91%
Literature References: Oxepane diterpenoid isolated from the leaves of the zoapatle plant, Montanoa tomentosa, Compositeae, which has been used by Mexican women to prepare "tea" to induce menses and labor. Isoln and structure: M. P. Wachter, R. M. Kanojia, US 4086358 (1978 to Ortho); S. D. Levine et al., J. Am. Chem. Soc. 101, 3404 (1979); R. M. Kanojia et al., J. Org. Chem. 47, 1310 (1982). Spasmogenic effects: J. B. Smith et al., Life Sci. 28, 2743 (1981). Total syntheses of (±)-form: R. Chen, D. A. Rowand, J. Am. Chem. Soc. 102, 6609 (1980); K. C. Nicolau et al., ibid. 6611; V. V. Kane, D. L. Doyle, Tetrahedron Lett. 22, 3027, 3031 (1981). Mass spec: C. J. Shaw, Org. Mass Spectrom. 16, 281 (1981). 13C-NMR study: M. L. Cotter, Org. Magn. Reson. 17, 14 (1981).

Pyridinium Chlorochromate CAS Registry Number: 26299-14-9 氯铬酸吡啶盐

CAS Name: Chlorotrioxochromate(1-), hydrogen, compd with pyridine (1:1)
Additional Names: PCC
Percent Composition: C 27.86%, H 2.81%, Cl 16.45%, Cr 24.12%, N 6.50%, O 22.27%
Literature References: Oxidizing agent for the efficient conversion of primary or secondary alcohols to carbonyl compounds. Prepn: R. J. Meyer, H. Best, Z. Anorg. Allg. Chem. 22, 192 (1899); J. Bernard, M. Camelot, C.R. Hebd. Seances Acad. Sci. 258, 5881 (1964); and use as an oxidant: E. J. Corey, J. W. Suggs, Tetrahedron Lett. 1975, 2647. Improved prepn: S. Agarwal et al., Tetrahedron 46, 4417 (1990). Oxidation, ring enlargement of furans to pyranones: G. Piancatelli et al., Tetrahedron Lett. 1977, 2199; oxidation of tertiary allylic alcohols: W. G. Dauben, D. M. Michno, J. Org. Chem. 42, 682 (1977). Role in oxidative cationic cyclization: E. J. Corey, D. L. Boger, Tetrahedron Lett. 1978, 2461. Review: G. Piancatelli et al., Synthesis 1982, 245-258.

Vedejs Reagent CAS Registry Number: 23319-63-3 韦德伊斯试剂

CAS Name: (PB-7-34-1222'2')-(Hexamethylphosphoric triamide-kO)oxodiperoxy(pyridine)molybdenum
Additional Names: oxodiperoxymolybdenum(pyridine)(hexamethylphosphoric triamide); MoOPH
Percent ...
Literature References: Oxidizing agent. Prepn and structural characterization: H. Mimoun et al., Bull. Soc. Chim. Fr. 1969, 1481. Prepn and synthetic use in hydroxylation of enolates: E. Vedejs, J. Am. Chem. Soc. 96, 5944 (1974); idem et al., J. Org. Chem. 43, 188 (1978); E. Vedejs, S. Larsen, Org. Synth. 64, 127 (1986). Improved prepn: A. R. Daniewski, W. Wojciechowska, Synth. Commun. 16, 535 (1986). Synthetic applications: K. Krohn et al., Ber. 123, 1729 (1990); K. Makino et al., Tetrahedron 58, 9737 (2002). Brief review: D. B. Weibel, Synlett 2000, 1076.

Thallium Trinitrate CAS Registry Number: 13746-98-0

CAS Name: Nitric acid thallium (3+) salt
Additional Names: thallium(III) nitrate
Percent Composition: Tl 52.35%, N 10.76%, O 36.88%
Literature References: Oxidizing reagent. Prepn and use for olefin rearrangement: A. McKillop et al., Tetrahedron Lett. 1970, 5275. Review of early uses: idem, E. C. Taylor, Endeavour 35, 88-93 (1976). Phenolic oxidation for isodityrosine functionality: K. Nakamura et al., Tetrahedron Lett. 42, 6311 (2001); promotion of ring contractions for indans: H. M. C. Ferraz et al., Tetrahedron 57, 1709 (2001). Review: idem et al., Synthesis 1999, 2001-2023; T. O. Vieira, Synlett 2002, 1017-1018.

Paraherquamide CAS Registry Number: 77392-58-6

Additional Names: (-)-Paraherquamide; [1'R-(1'a,5'ab,7'b,8'ab,9'ab)]-2',3',8'a,9'-tetrahydro-1'-hydroxy-1',4,4,8',8',11'-hexamethylspiro[4H,8H-[1,4]dioxepino[2,3-g]indole-8,7'(8'H)-[5H,6H-5a,9a](i...
Literature References: Oxindole alkaloid fungal metabolite. Isolation from Penicillium paraherquei and structure: M. Yamazaki et al., Maikotokishin 10, 27 (1980), C.A. 95, 19321p (1981); M. Yamazaki et al., Tetrahedron Lett. 22, 135 (1981); from P. charlesii and nematocidal activity: J. G. Ondeyka et al., J. Antibiot. 43, 1375 (1990). Absolute stereochemistry: T. A. Blizzard et al., J. Org. Chem. 54, 2657 (1989). Approach to synthesis: R. M. Williams, T. D. Cushing, Tetrahedron Lett. 31, 6325 (1990). Anthelmintic activity in sheep: W. L. Shoop et al., J. Parasitol. 76, 349 (1990); in dogs: W. L. Shoop et al., Vet. Parasitol. 40, 339 (1991). Toxicity: eidem, Am. J. Vet. Res. 53, 2032 (1992). Mode of action: J. M. Schaeffer et al., Biochem. Pharmacol. 43, 679 (1992).

Flufenacet CAS Registry Number: 142459-58-3 氟噻草胺

CAS Name: N-(4-Fluorophenyl)-N-(1-methylethyl)-2-[[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]oxy]acetamide
Additional Names: N-isopropyl-(5-trifluoromethyl-1,3,4-thiadiazol-2-yl)-(4'-fluorooxya...
Literature References: Oxyacetamide herbicide. Prepn: H. Förster et al., DE 3821600; eidem, US 4968342 (1989, 1990 both to Bayer). Ecotoxicological profile: T. Hall, Pflanzenschutz-Nachr. Bayer (Engl. Ed.) 50, 187 (1997). Series of articles on chemical and biological properties, determn and field trials: ibid. 105-236. Review of properties and grass control in crops: R. Deege et al., Brighton Crop Prot. Conf. - Weeds 1995, 43.

Etanidazole CAS Registry Number: 22668-01-5 依他硝唑

CAS Name: N-(2-Hydroxyethyl)-2-nitro-1H-imidazole-1-acetamideTrademarks: Radinyl (Roberts)
Percent Composition: C 39.25%, H 4.71%, N 26.16%, O 29.88%
Literature References: Oxygen-mimetic which renders hypoxic cells sensitive to chemo- and radiotherapy. Prepn: A. G. Beaman et al., Antimicrob. Agents Chemother. 1967, 520. See also: W. W. Lee et al., US 4371540 (1983 to U.S. Sec'y Health Human Serv.). Pharmacology: J. M. Brown et al., Int. J. Radiat. Oncol. Biol. Phys. 7, 695 (1981). HPLC determn in biological materials: R. Ward, P. Workman, J. Chromatogr. 420, 223 (1987). Clinical pharmacokinetics and efficacy in radiation therapy: T. H. Wasserman et al., Radiother. Oncol. 20, Suppl. 1, 129 (1991). Evaluation in combination with alkylating agents: L. N. Shulman et al., Int. J. Radiat. Oncol. Biol. Phys. 29, 545 (1994).

Acetanilide CAS Registry Number: 103-84-4 N-乙酰苯胺

CAS Name: N-Phenylacetamide
Additional Names: antifebrin; acetylaniline; acetylaminobenzene
Percent Composition: C 71.09%, H 6.71%, N 10.36%, O 11.84%
Literature References: p-Aminophenol deriv related to acetaminophen, q.v., with analgesic and antipyretic properties. Usually prepd from aniline and acetic acids: A. I. Vogel, Practical Organic Chemistry (London, 3rd ed., 1959) p 577. From aniline and acetyl chloride: Gattermann-Wieland, Praxis des Organischen Chemikers (Berlin, 40th ed., 1961) p 114. From aniline, acetone and ketene: Hurd, Org. Synth. coll. vol. I (New York, 2nd ed., 1941) p 332. Chemistry: G. C. Derick, J. H. Bornman, J. Am. Chem. Soc. 35, 1269 (1913). Toxicity data: P. K. Smith, W. E. Hambourger, J. Pharmacol. Exp. Ther. 54, (1935). Monograph: Gross, Acetanilid (Hillhouse Press, New Haven, 1946).

Orlistat CAS Registry Number: 96829-58-2 奥利司他

CAS Name: N-Formyl-L-leucine (1S)-1-[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl ester
Additional Names: N-formyl-L-leucine ester with (3S,4S)-3-hexyl-4-[(2S)-2-hydroxytridecyl]-2-oxetanon...
Literature References: Pancreatic lipase inhibitor. Isoln from fermentation broth of Streptomyces toxytricini: P. Hadvary et al., EP 129748; eidem, US 4598089 (1985, 1986 both to Hoffmann-LaRoche). Structural elucidation: E. Hochuli et al., J. Antibiot. 40, 1086 (1987). Synthesis and absolute configuration: P. Barbier, F. Schneider, Helv. Chim. Acta 70, 196 (1987). Total synthesis: S. Hanessian et al., J. Org. Chem. 58, 7768 (1993). Mechanism of action: B. Borgström, Biochim. Biophys. Acta 962, 308 (1988). Clinical pharmacology: J. B. Hauptman et al., Am. J. Clin. Nutr. 55, 309S (1992). Clinical trial: M. H. Davidson et al., J. Am. Med. Assoc. 281, 235 (1999). Review of pharmacology and clinical efficacy in treatment of obesity: W. McNeely, P. Benfield, Drugs 56, 241-249 (1998). Evaluation of long-term efficacy and tolerability: J. Hauptman et al., Arch. Fam. Med. 9, 160 (2000).