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

Deslorelin CAS Registry Number: 57773-65-6 德舍瑞林

CAS Name: 6-D-Tryptophan-9-(N-ethyl-L-prolinamide)-10-deglycinamideluteinizing hormone-releasing factor (pig)
Additional Names: [D-Trp6,des-Gly10]-LH-RH ethylamide
Trademarks: Somagard (Robe...
Literature References: Synthetic nonapeptide agonist analog of LH-RH, q.v. Prepn: D. H. Coy et al., J. Med. Chem. 19, 423 (1976); W. Kornreich et al., Int. J. Pept. Protein Res. 25, 414 (1985). Pharmacology: K. Sundaram et al., Life Sci. 28, 83 (1981). Pharmacokinetics and metabolism: B. Candas et al., J. Clin. Endocrinol. Metab. 70, 1046 (1990). Clinical inhibition of spermatogenesis: R. Linde et al., N. Engl. J. Med. 305, 663 (1981). Clinical trial in combination with flutamide, q.v., for prostatic carcinoma: A. Dupont et al., Eur. J. Cancer Clin. Oncol. 24, 659 (1988). Clinical evaluation in precocious puberty: P. K. Manasco et al., J. Pediatr. 115, 105 (1989).

Histrelin CAS Registry Number: 76712-82-8 组氨瑞林

CAS Name: 6-[1-(Phenylmethyl)-D-histidine]-9-(N-ethyl-L-prolinamide)-10-deglycinamide luteinizing hormone-releasing factor (pig)
Additional Names: 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl...
Literature References: Synthetic nonapeptide agonist analog of LH-RH, q.v. Prepn: J. E. F. Rivier, W. W. Vale, Jr., EP 21620; eidem, US 4244946 (both 1981 to Salk Inst.). See also: J. E. Rivier, W. W. Vale, Life Sci. 23, 869 (1978). Pharmacology: Y-Q. Cao et al., Int. J. Androl. 5, 158 (1982); J. W. Gunnet et al., J. Endocrinol. 131, 211 (1991). HPLC purification: J. Rivier et al., J. Chromatogr. 288, 303 (1984). Amino acid sequence: C. J. Shaw, M. L. Cotter, Chromatographia 21, 197 (1986). Clinical evaluations in polycystic ovarian disease: K. Steingold et al., J. Clin. Endocrinol. Metab. 65, 773 (1987); in endometriosis: idem et al., Obstet. Gynecol. 69, 403 (1987); in porphyria: K. E. Anderson et al., Arch. Int. Med. 150, 1469 (1990); in PMS: J. F. Mortola et al., J. Clin. Endocrinol. Metab. 72, 252A (1991). Review of pharmacology and therapeutic use in central precocious puberty: L. B. Barradell, D. McTavish, Drugs 45, 570-588 (1993).

Leuprolide CAS Registry Number: 53714-56-0 亮丙瑞林

CAS Name: 6-D-Leucine-9-(N-ethyl-L-prolinamide)-10-deglycinamideluteinizing hormone-releasing factor (pig)
Additional Names: leuprorelin; (D-Leu6)-des-Gly10-LH-RH-ethylamide
Percent Composit...
Literature References: Synthetic nonapeptide agonist analog of LH-RH, q.v. Prepn: M. Fujino et al., DE 2446005 (1975 to Takeda), C.A. 83, 10895y (1975); R. L. Gendrich et al., US 4005063 (1977 to Abbott). Synthesis: J. A. Vilchez-Martinez et al., Biochem. Biophys. Res. Commun. 59, 1226 (1974); M. Fujino et al., ibid. 60, 406 (1974). Comparison of biological activity with natural LH-RH: D. H. Coy et al., ibid. 67, 576 (1975). Pharmacokinetics: L. T. Sennello et al., J. Pharm. Sci. 75, 158 (1986). Clinical efficacy in prostatic carcinoma: M. B. Garnick et al., N. Engl. J. Med. 311, 1281 (1984); in benign prostatic hypertrophy: L. M. Eri, K. J. Tveter, J. Urol. 150, 359 (1993). Clinical trial in endometriosis: J. M. Wheeler et al., Am. J. Obstet. Gynecol. 167, 1367 (1992).

Buserelin CAS Registry Number: 57982-77-1 布舍瑞林

CAS Name: 6-[O-(1,1-dimethylethyl)-D-serine]-9-(N-ethyl-L-prolinamide)-10-deglycinamideluteinizing hormone-releasing factor (pig)
Percent Composition: C 58.14%, H 6.99%, N 18.08%, O 16.78%
Literature References: Synthetic nonapeptide agonist analog of LH-RH, q.v. Synthesis: W. Konig et al., DE 2438350; eidem, US 4024248 (1976, 1977 both to Hoechst); A. S. Dutta et al., J. Med. Chem. 21, 1018 (1978). Clinical pharmacology: A. Lemay et al., Fertil. Steril. 37, 193 (1982). Radioimmunoassay in plasma and urine: S. Saito et al., J. Immunol. Methods 79, 173 (1985). Veterinary use to increase conception rate: K. Moller, E. D. Fielden, N. Z. Vet. J. 29, 214 (1981). Clinical evaluation in prostatic carcinoma: J. H. Waxman, Br. J. Urol. 55, 737 (1983); as ovulatory stimulant for in vitro fertilization: V. MacLachlan et al., N. Engl. J. Med. 320, 1233 (1989). Review of pharmacokinetics and clinical profile: R. N. Brogden et al., Drugs 39, 399-437 (1990); of efficacy in prostatic carcinoma: H. J. de Voogt et al., Scand. J. Urol. Nephrol. Suppl 138, 131-136 (1991).

Fertirelin CAS Registry Number: 38234-21-8 夫替瑞林

CAS Name: 9-(N-Ethyl-L-prolinamide)-1-9-luteinizing hormone-releasing factor (swine)
Additional Names: 9-(N-ethyl-L-prolinamide)-10-deglycinamide-luteinizing hormone-releasing factor (pig); Des...
Literature References: Synthetic nonapeptide analog of LH-RH, q.v. Prepn: M. Fujino et al., DE 2321174; eidem, US 3853837 (1973, 1974 both to Takeda); S. Shinagawa, M. Fujino, Chem. Pharm. Bull. 23, 229 (1975); see also: M. Fujino et al., Biochem. Biophys. Res. Commun. 49, 863 (1972). Enzyme immunoassay in bovine plasma: J. Okada, S. Kondo, ibid. 33, 4464 (1985). HPLC determn of bulk drugs and formulations: P. A. Hartman, J. D. Stodola, J. Chromatogr. 444, 177 (1988). Field trial in bovine cystic ovarian disease: T. Nakao et al., Jpn. J. Vet. Sci. 45, 269 (1983); to induce ovulation for insemination of dairy cows: T. Nakao et al., Theriogenology 20, 111 (1983); K. Yamada et al., Anim. Reprod. Sci. 74, 27 (2002).

Methoxyfenozide CAS Registry Number: 161050-58-4 甲氧虫酰肼

CAS Name: 3-Methoxy-2-methylbenzoic acid 2-(3,5-dimethylbenzoyl)-2-(1,1-dimethylethyl)hydrazide
Additional Names: N'-tert-butyl-N'-(3,5-dimethylbenzoyl)-3-methoxy-2-methylbenzohydrazide; N-tert...
Literature References: Synthetic nonsteroidal ecdysone agonist. Prepn: Z. Lidert et al., EP 602794; eidem, US 5530028 (1994, 1996 both to Rhom Haas). Comparative insecticidal activity: A. Trisyono, G. M. Chippendale, J. Econ. Entomol. 90, 1486 (1997). Mechanism of action and metabolism: G. Smagghe et al., Pestic. Sci. 55, 386 (1999). Review of physical properties, biological activity and field studies: D. P. Le et al., Brighton Crop Prot. Conf. - Pests Dis. 1996, 481-486; of physical properties and insecticidal activity: G. R. Carlson et al., Pest Manage. Sci. 57, 115-119 (2001).

Troxacitabine CAS Registry Number: 145918-75-8 4-氨基-1-[(2S)-2-(羟甲基)-1,3-二氧杂环戊-4-基]嘧啶-2-酮

CAS Name: 4-Amino-1-[(2S,4S)-2-(hydroxymethyl)-1,3-dioxolan-4-yl]-2(1H)-pyrimidinone
Additional Names: (-)-2'-deoxy-3'-oxacytidine; b-L-(-) dioxolane cytidine; (-)-(2S,4S)-1-[2-(hydroxymethyl)-...
Literature References: Synthetic nucleoside analog with stereochemically unnatural b-L configuration. Prepn: Y.-C. Cheng et al., WO 9218517 (1992 to Yale Univ. and Univ. Georgia Res. Found.); B. R. Belleau et al., Tetrahedron Lett. 33, 6949 (1992); H. O. Kim et al., J. Med. Chem. 36, 519 (1993). Resolution of enantiomers: M. P. DiMarco et al., J. Chromatogr. 645, 107 (1993). Structure activity study: T. S. Mansour et al., Nucleosid. Nucleotid. 14, 627 (1995). Clinical pharmacokinetics: J. S. deBono et al. J. Clin. Oncol. 20, 96 (2001). Population pharmacokinetics: C. K. K. Lee et al., Clin. Cancer Res. 12, 2158 (2006). Clinical evaluation in refractory leukemia: F. J. Giles et al., ibid. 20, 656 (2002); in imatinib-resistant chronic myelogenous leukemia: idem et al., Leukem. Res. 27, 1091 (2003); in pancreatic cancer: R. Lapointe et al., Ann. Oncol. 16, 289 (2005). Review of pharmacology and clinical development: idem, Expert Rev. Anticancer Ther. 2, 261-266 (2002); G. Ecker, Curr. Opin. Invest. Drugs 3, 1533-1538 (2002).

Altrenogest CAS Registry Number: 850-52-2 烯丙孕素

CAS Name: (17b)-17-Hydroxy-17-(2-propenyl)estra-4,9,11-trien-3-one
Additional Names: 17a-allyl-17-hydroxyestra-4,9,11-trien-3-one; 13b-methyl-17a-allyl-D4,9,11-gonatriene-17b-ol-3-one; allytren...
Literature References: Synthetic oral progestogen. Prepn: NL 6401555; G. Nomine et al., US 3257278 (1964, 1966 both to Roussel). Effect on estrous cycle and fertility of mares: E. L. Squires et al., J. Anim. Sci. 49, 729 (1979). Synchronization of estrus in swine: R. R. Kraeling et al., ibid. 52, 831 (1981); in gilts: V. G. Pursel et al., ibid. 130.

p-Cresyl Phenylacetate CAS Registry Number: 101-94-0 苯乙酸对甲苯酯

CAS Name: Benzeneacetic acid 4-methylphenyl ester
Additional Names: p-tolyl phenylacetate
Percent Composition: C 79.62%, H 6.24%, O 14.14%
Literature References: Synthetic organic ester in perfumery. Prepn: W. Autenrieth, G. Thomae, Ber. 57, 423 (1924). Fragrance monograph: Food Cosmet. Toxicol. 13, 775 (1975). Photochemistry study: C.-H. Tung, Y.-M. Ying, J. Chem. Soc. Perkin Trans. 2 1997, 1319. Synthesis using montmorillonite catalysts: C. R. Reddy et al., J. Mol. Catal. A 223, 117 (2004). Environmentally benign synthesis of perfumery grade product: G. D. Yadav, S. V. Lande, Org. Process Res. Dev. 9, 288 (2005).

Pentigetide CAS Registry Number: 62087-72-3 喷替吉肽

CAS Name: N2-[1-[N-(N-L-a-Aspartyl-L-seryl)-L-a-aspartyl]-L-prolyl]-L-arginine
Additional Names: human IgE pentapeptide; HEPP
Trademarks: Pentyde (Immunetech)
Percent Composition: C 44.89...
Literature References: Synthetic pentapeptide with antiallergic activity. Structure corresponds to amino acids 320-324 of the epsilon chain of human immunoglobulin E (IgE). Prepn: R. N. Hamburger, DE 2602443; idem, US 4171299 (1976, 1979 both to Univ. California). Inhibition of IgE-mediated immediate hypersensitivity response: idem, Science 189, 389 (1975). Stimulation of peritoneal macrophages: E. Tzehoval et al., Proc. Natl. Acad. Sci. USA 75, 3400 (1978). Mechanism of action study: R. N. Hamburger, Immunology 38, 781 (1979). Clinical evaluations in allergic rhinitis: G. A. Cohen et al., Ann. Allergy 52, 83 (1984); B. M. Prenner, ibid. 58, 332 (1987).