CAS: 40432-52-8; 3-Amino-1-(Diphenylmethyl)Azetidine

上下游产品

CAS号38353-74-1 benzhydryl-1 ph... | CAS号33301-41-6 1-二苯甲基-3-甲烷磺酸氮杂环丁烷 | CAS号91189-18-3 (1-苯甲酰基氮杂环丁烷-3-... | CAS号18621-17-5 N-二苯甲基氮杂环丁烷-3-醇 | CAS号91-00-9 二苯甲胺 | CAS号63477-43-0 1-(二苯甲基氨基)-3-氯丙烷-2-醇 | CAS号40320-60-3 1-二苯甲基氮杂环丁烷-3-酮 | CAS号91189-18-3 (1-苯甲酰基氮杂环丁烷-3-...

1-二苯甲基-3-甲烷磺酸氮杂环丁烷置于sodium Azide,氯化铵,锌体系中,用 乙醇,水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 7.0H,反应生成 3-氨基-1-二苯甲基氮杂环丁烷
参考文献:新型氮杂环丁烷衍生物作为多巴胺拮抗剂的合成及生物学评价
标题:新型氮杂环丁烷衍生物作为多巴胺拮抗剂的合成及生物学评价
摘要:在这项研究中,评估了氮杂环丁烷衍生物作为多巴胺能拮抗剂的功效.该研究包括在3位上被酰胺部分取代的衍生物.此外,酰胺的苯基部分在2,3或4位被修饰.对取代的化合物对d 2和d 4受体的亲和力进行生物学评估.这些化合物中最有效的d 2和d 4拮抗剂似乎是n-(1-苯甲酰基-氮杂环丁烷-3Yl)-2-溴-苯甲酰胺和n-(1-苯甲酰基-氮杂环丁烷-3Yl)-4-溴-苯甲酰胺.cppma与d 4受体的各种对接相互作用和化合物5的相同,即n发现-(1-苯甲酰基-氮杂环丁烷-3Yl)-4-溴-苯甲酰胺与观测到的生物活性具有非常好的相关性.
DOI:10.1007/s00044-013-0579-3

专利信息

专利号:US-4943641-A
优先权日:1984-02-27
标 题:3-aminoazetidine, its salts, process for their preparation and intermediates of synthesis
发明人：NISATO DINO; FRIGERIO MARCO
权利人:SANOFI SA
摘要:The 3-aminoazetidine, its salts, new intermediates of formula wherein X' represents hydrogen or a protecting group and both X'' represent hydrogen or, together with the nitrogen atom, a phthalimido group, X' not and both X'' being hydrogen at the same time; a process for the preparation of the 3-aminoazetidine, starting from a 1-protected 3-sulfonyloxyazetidine by reaction with the potassium phthalimide and transformation of the above mentioned intermediates.

专利号:CN-119751326-A
优先权日:2024-11-26
标题:A method for high-throughput synthesis of 1-phenylazetidine compounds

专利号:US-6214832-B1
优先权日:1997-06-18
标 题 :Bis-piperidinyl-pyrimidin-2-ones as alpha 1a adrenergic receptor antagonists
发明人：PATANE MICHAEL A; BOCK MARK G
权利人:MERCK & CO INC
摘要:Pyrimidinone, oxazolidinone, and (alkyl)aryl derivatives, their synthesis, and their use as alpha 1a adrenergic receptor antagonists are disclosed. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved. Among the disclosed derivatives are piperidinyl aminoalkylpiperidinyl pyrimidinones, including those of formula:R1 is selected from unsubstituted, mono- or poly-substituted phenyl wherein the substituents on the phenyl are independently selected from halogen, CF3, cyano, nitro, N(R7)2, NR7COR19, NR7CON(R19)2, NR7SO2R19, NR7SO2N(R19)2, OR6, (CH2)0-4CO2R7, (CH2)0-4CON(R7)2, or C1-4 alkyl; or unsubstituted, mono- or poly-substituted pyridyl, pyrazinyl, thienyl, thiazolyl, furanyl, quinazolinyl or naphthyl wherein the substituents on the pyridyl, pyrazinyl, thienyl, thiazolyl, furanyl, quinazolinyl or naphthyl are independently selected from CF3, cyano, nitro, amino, (CH2)0-4CO2R7, (CH2)0-4CON(R7)2, (CH2)0-4SO2N(R7)2, (CH2)0-4SO2R6, phenyl, OR6, halogen, C1-4 alkyl or C3-8 cycloalkyl;m and p are each integers from zero to two, wherein the sum m+p=2; n and o are each integers from zero to two, wherein the sum n+o=2; q is an integer of from zero to three, provided that when q is zero, R26 is hydrogen; s is an integer of from zero to four; andE, G, J, L, M, W, X, R2, R3, R4, R5, R6, R7, R8, R11, R12, R13, R14, R15, R16, R19 and R26 are defined herein.

专利号:US-6080760-A
优先权日:1997-06-18
标题:Alpha 1A adrenergic receptor antagonists
发明人：PATANE MICHAEL A; BOCK MARK G
权利人:MERCK & CO INC
摘要:This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

专利号:WO-9857642-A1
优先权日:1997-06-18
标题:ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS
发明人：PATANE MICHAEL A; BOCK MARK G
权利人:MERCK & CO INC; PATANE MICHAEL A; BOCK MARK G
摘要:This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

专利号:US-6143750-A
优先权日:1997-06-18
标 题 :Alpha 1a adrenergic receptor antagonists
发明人：PATANE MICHAEL A; BOCK MARK G
权利人:MERCK & CO INC
摘要:This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.