公开(公告)号：US4847401A

公开(公告)日：1989-07-11

申请号：US145694

申请日：1988-01-15

Applicant: Fritz Gerhart ,  Michael Kolb

Inventor： Fritz Gerhart ,  Michael Kolb

IPC: B01J19/00 ,  B01J19/18

CPC classification number: B01J19/0013 ,  B01J19/18 ,  B01J2219/00058

Abstract: The large scale preparation of ethyl 2,2-difluoro-4- pentenoate and 2-fluorinated methyl aminoacetonitriles by reaction of 2-H-perfluoroethyl allyl ether and n-butyl lithium and fluoromethylacetonitrile and a Grignard reagent, respectively, is largly unsuccessful because of side reactions which convert intermediate products and reactants to undesired products. Applicants have overcome these problems by performing the reactions with cooling in a continuous manner in a flow reactor with short residence time.

Abstract translation: 通过2-H-全氟乙基烯丙基醚和正丁基锂和氟甲基乙腈和格氏试剂的反应分别大规模制备2,2-二氟-4-戊烯酸乙酯和2-氟化甲基氨基乙腈，这是因为 将中间产物和反应物转化为不期望的产物的副反应。 申请人通过在具有短停留时间的流动反应器中连续冷却进行反应来克服这些问题。

公开(公告)号：US4374128A

公开(公告)日：1983-02-15

申请号：US243280

申请日：1981-03-13

Applicant: Philippe Bey ,  Michel Jung ,  Michael Kolb ,  Charles Danzin

Inventor： Philippe Bey ,  Michel Jung ,  Michael Kolb ,  Charles Danzin

IPC: A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7076 ,  A61P33/02 ,  A61P35/00 ,  C07H19/16 ,  C07H19/167

CPC classification number: C07H19/16 ,  C07C255/00

Abstract: Novel compounds of the following general Formula I are useful pharmacological agents: ##STR1## wherein: Ado represents 5'-deoxyadenosin-5'-yl;R.sub.1 represents methyl, ethyl or, preferably hydrogen;R.sub.2 represents C.sub.1 -C.sub.8 alkylene;R.sub.4 represents C.sub.1 -C.sub.8 alkylene;R.sub.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl or --R.sub.6 NHR.sub.7 ;R.sub.6 represents C.sub.1 -C.sub.4 alkylene; andR.sub.7 represents hydrogen or C.sub.1 -C.sub.6 alkyl;and pharmaceutically acceptable acid addition salts thereof.

Abstract translation: 以下通式I的新化合物是有用的药理学药剂：其中：Ado代表5'-脱氧腺苷酸-5'-基; R 1表示甲基，乙基或优选氢; R2代表C1-C8亚烷基; R4代表C1-C8亚烷基; R5表示氢，C1-C6烷基或-R6NHR7; R6表示C1-C4亚烷基; 并且R 7表示氢或C 1 -C 6烷基; 及其药学上可接受的酸加成盐。