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

Tuaminoheptane CAS Registry Number: 123-82-0 2-氨基庚烷

CAS Name: 2-Heptanamine
Additional Names: 1-methylhexylamine; 2-aminoheptane
Trademarks: Tuamine (Lilly)
Percent Composition: C 72.97%, H 14.87%, N 12.16%
Literature References: a-Adrenergic agonist; topical vasoconstrictor. Prepd by heating 2-bromoheptane on steam bath with alcoholic ammonia in pressure tube: Clarke, J. Am. Chem. Soc. 21, 1027 (1899); by hydrogenation of methyl amyl ketone and ammonia in the presence of Raney nickel: Norton et al., J. Org. Chem. 19, 1054 (1954).

Xylometazoline CAS Registry Number: 526-36-3 木霉唑啉

CAS Name: 2-[[4-(1,1-Dimethylethyl)-2,6-dimethylphenyl]methyl]-4,5-dihydro-1H-imidazole
Additional Names: 2-(4-tert-butyl-2,6-dimethylbenzyl)-2-imidazoline
Percent Composition: C 78.64%, H 9...
Literature References: a-Adrenergic agonist; topical vasoconstrictor. Prepn: Hüni, US 2868802 (1959 to Ciba). Pharmacology: S. Morimoto, H. Tanaka, Osaka-shiritsu Daigaku Igaku Zasshi 18, 211 (1969), C.A. 72, 20437n (1970). Comprehensive description: Y. Golander, W. J. DeWitte, Anal. Profiles Drug Subs. 14, 135-156 (1985). GC determn in plasma and urine: A. Sioufi et al., J. Chromatogr. 487, 81 (1989). Clinical trial in allergic rhinitis: M. Fradis et al., J. Laryngol. Otol. 101, 666 (1987); in nasal surgery: J. P. Campbell et al., Otolaryngol. Head Neck Surg. 107, 697 (1992).

Dihydroergotamine CAS Registry Number: 511-12-6 双氢麦角胺

CAS Name: 9,10-Dihydro-12'-hydroxy-2'-methyl-5'-(phenylmethyl)ergotaman-3',6',18-trione
Percent Composition: C 67.91%, H 6.39%, N 12.00%, O 13.71%
Literature References: a-Adrenergic blocker with selective venoconstrictor properties. Also binds to serotonin 5HT1-receptors. Prepn from ergotamine: Stoll, Hofmann, Helv. Chim. Acta 26, 2070 (1943). Clinical pharmacology: H. de Marées et al., Eur. J. Clin. Pharmacol. 30, 685 (1986). Neurotransmitter receptor binding study: B. G. McCarthy, S. J. Peroutka, Headache 29, 420 (1989). Clinical trials in migraine: P. Winner et al., ibid. 33, 471 (1993); D. Ziegler et al., Neurology 44, 447 (1994).

Fenspiride CAS Registry Number: 5053-06-5 芬司匹利

CAS Name: 8-(2-Phenylethyl)-1-oxa-3,8-diazaspiro[4.5]decan-2-one
Additional Names: decaspiride; DESP
Percent Composition: C 69.20%, H 7.74%, N 10.76%, O 12.29%
Literature References: a-Adrenergic blocker. Prepn: NL 6504602; Regnier et al., US 3399192 (1965 and 1968, both to Sci. Union et Cie-Soc. Franc. Recherche Méd.). Pharmacology: LeDouarec et al., Arzneim.-Forsch. 19, 1263 (1969); Duhault et al., ibid. 22, 1947 (1972).

Piperoxan CAS Registry Number: 59-39-2 1-[(2,3-二氢-1,4-苯并二氧杂环己-2-基)甲基]哌啶

CAS Name: 1-[(2,3-Dihydro-1,4-benzodioxin-2-yl)methyl]piperidine
Additional Names: 2-piperidinomethyl-1,4-benzodioxan; 2-(1-piperidylmethyl)-1,4-benzodioxan; benzodioxane
Trademarks: Benodai...
Literature References: a-Adrenergic blocker. Prepn: Fourneau, US 2056046 (1936 to Rhône-Poulenc).

Phentolamine CAS Registry Number: 50-60-2 酚妥拉明

CAS Name: 3-[[(4,5-Dihydro-1H-imidazol-2-yl)methyl](4-methylphenyl)amino]phenol
Additional Names: 2-[N-(m-hydroxyphenyl)-p-toluidinomethyl]imidazoline; 2-(m-hydroxy-N-p-tolylanilinomethyl)-2-im...
Literature References: a-Adrenergic blocker. Prepn: K. Miescher et al., US 2503059 (1950 to Ciba); E. Urech et al., Helv. Chim. Acta 33, 1386 (1950). Pharmacology and toxicity: R. Meier et al., Proc. Soc. Exp. Biol. Med. 71, 70 (1949). HPLC determn in biological samples: B. D. Kerger et al., Anal. Biochem. 170, 145 (1988). Diagnostic use: G. Spergel et al., J. Am. Med. Assoc. 211, 266 (1970). Review of pharmacology and therapeutic applications: L. Gould, C. V. R. Reddy, Am. Heart J. 92, 397-402 (1976). Clinical efficacy of combination with papaverine in impotence: A. Bechara et al., J. Urol. 157, 2132 (1997).

N-(2-Chloroethyl)dibenzylamine Hydrochloride CAS Registry Number: 55-43-6 N-(2-氯乙基)二苄胺盐酸盐

CAS Name: N-(2-Chloroethyl)-N-(phenylmethyl)benzenemethanamine hydrochloride
Additional Names: N,N-dibenzyl-b-chloroethylamine hydrochloride; N,N-dibenzylaminoethyl chloride hydrochloride
Tr...
Literature References: a-Adrenergic blocker. Prepn: Rabald, Dimroth, DE 824208 (1951 to Boehringer, Mann.), C.A. 47, 2206 (1953). Pharmacology and toxicity: M. Nickerson, G. M. Nomaguchi, J. Pharmacol. Exp. Ther. 101, 379 (1951). Use in adrenergic receptor differentiation: R. F. Furchgott, ibid. 111, 265 (1954); in specific receptor labelling: R. D. Green et al., ibid. 187, 524 (1973). In vivo studies of protection against hepatotoxic agents: H. M. Maling et al., Toxicol. Appl. Pharmacol. 27, 380 (1974); E. K. Weisburger et al., ibid. 28, 477 (1974); H. M. Maling et al., Biochem. Pharmacol. 23, 1479 (1974).

Tolazoline CAS Registry Number: 59-98-3 2-苄基咪唑啉

CAS Name: 4,5-Dihydro-2-(phenylmethyl)-1H-imidazole
Additional Names: 2-benzyl-2-imidazoline; 2-benzyl-2-iminazoline; benzazoline; 2-benzyl-4,5-imidazoline; phenylmethylimidazoline
Percent C...
Literature References: a-Adrenergic blocker. Prepn: Sonn, US 2161938 (1939 to Ciba). HPLC determn in serum: L. M. L. Todesco et al., Ther. Drug Monit. 9, 78 (1987). Review of pharmacology and clinical use: R. M. Ward, Clin. Perinatol. 11, 703-713 (1984).

a -Carotene CAS Registry Number: 7488-99-5 α-胡萝卜素

Percent Composition: C 89.49%, H 10.51%
Literature References: About as widely distributed as its b-isomer, but in smaller amounts. Best sources for both the a- and b-isomers are carrots, palm oil, and green leaves of various species. As a provitamin A it is half as active as b-carotene. Found in the mother liquors after crystallizing b-carotene. Isoln by chromatography: Karrer, Walker, Helv. Chim. Acta 16, 641 (1933). Structure: Kuhn, Lederer, Ber. 64, 1349 (1931); Karrer et al., Helv. Chim. Acta 14, 614 (1931); 16, 975 (1933). Natural (+)-a-carotene has 6¢R configuration: Eugster et al., ibid. 52, 1729 (1969). Synthesis of dl-a-carotene: Eugster, Karrer, ibid. 38, 610 (1955); Tscharner et al., ibid. 40, 1676 (1957); Ruegg et al., ibid. 44, 985 (1961).

Osteocalcin CAS Registry Number: 75757-02-7 (human reduced)

Additional Names: Bone Gla protein; BGP
Literature References: Abundant noncollagenous, calcium-binding protein of bone; constitutes ~1-2% of the total bone matrix. Also found in tooth dentin and cementum. Contains 46-50 amino acid residues (human: 49); mol wt ~5800 daltons. Amino acid sequence is highly conserved across species. Characterized by 3 residues of the vitamin K-dependent amino acid, g-carboxyglutamic acid (Gla), q.v. Synthesized by osteoblasts and odontoblasts; modulated by calcitriol, q.v. Detectable in serum as an indicator of bone metabolism. Identification in chicken bone: P. V. Hauschka et al., Proc. Natl. Acad. Sci. USA 72, 3925 (1975). Characterization of calf BGP: P. A. Price et al. ibid. 73, 1447 (1976). Biosynthesis in bone cell culture: S. K. Nishimoto, P. A. Price, J. Biol. Chem. 254, 437 (1979). RIA determn in plasma: P. A. Price et al., J. Clin. Invest. 66, 878 (1980). Review of isoln and characterization: C. M. Gundberg et al., Methods Enzymol. 107B, 516-544 (1984). Review of hydroxyapatite binding characteristics: P. V. Hauschka, F. H. Wians, Jr. Anat. Rec. 224, 180-188 (1989). Comprehensive review: P. V. Hauschka et al., Physiol. Rev. 69, 990-1047 (1989). Review of diagnostic methods and clinical applications: M. J. Power, P. F. Fottrell, Crit. Rev. Clin. Lab. Sci. 28, 287-335 (1991). Immunohistochemical study and potential role in bone mineralization and resorption: H. I. Roach, Cell Biol. Int. 18, 617-628 (1994).